An indole-dione that is obtained by oxidation of indigo blue. It is a MONOAMINE OXIDASE INHIBITOR and high levels have been found in urine of PARKINSONISM patients.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Analogs or derivatives of mandelic acid (alpha-hydroxybenzeneacetic acid).
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)
Acyclic branched or unbranched hydrocarbons having two carbon-carbon double bonds.
Derivatives and polymers of styrene. They are used in the manufacturing of synthetic rubber, plastics, and resins. Some of the polymers form the skeletal structures for ion exchange resin beads.
An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 1.4.3.4.
A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414)
An antidepressive agent and monoamine oxidase inhibitor related to PARGYLINE.
A monoamine oxidase inhibitor with antihypertensive properties.
A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson's disease. It may slow progression of the clinical disease and delay the requirement for levodopa therapy. It also may be given with levodopa upon onset of disability. (From AMA Drug Evaluations Annual, 1994, p385) The compound without isomeric designation is Deprenyl.
Detailed account or statement or formal record of data resulting from empirical inquiry.
A plant genus of the family GENTIANACEAE. Triterpene lactones and other compounds have been isolated from species of this genus. The common name of century plant has also been used for the AGAVE genus.
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.
Substances that reduce the growth or reproduction of BACTERIA.
Bacteria which retain the crystal violet stain when treated by Gram's method.
One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive.
Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method.
Four fused benzyl rings with three linear and one angular, that can be viewed as a benzyl-phenanthrenes. Compare with NAPHTHACENES which are four linear rings.
Activity involved in transfer of goods from producer to consumer or in the exchange of services.
Compounds that inhibit the activity of DNA TOPOISOMERASES.
Enzymes that regulate the topology of DNA by actions such as breaking, relaxing, passing, and rejoining strands of DNA in cells. These enzymes are important components of the DNA replication system. They are classified by their substrate specificities. DNA TOPOISOMERASE I enzymes act on a single strand of DNA. DNA TOPOISOMERASE II enzymes act on double strands of DNA.
An inhibitor of ALPHA-GLUCOSIDASES that retards the digestion and absorption of DIETARY CARBOHYDRATES in the SMALL INTESTINE.
An enzyme that catalyzes the endohydrolysis of 1,6-alpha-glucosidic linkages in isomaltose and dextrins produced from starch and glycogen by ALPHA-AMYLASES. EC 3.2.1.10.
Enzymes that catalyze the exohydrolysis of 1,4-alpha-glucosidic linkages with release of alpha-glucose. Deficiency of alpha-1,4-glucosidase may cause GLYCOGEN STORAGE DISEASE TYPE II.
Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Enzymes that hydrolyze O-glucosyl-compounds. (Enzyme Nomenclature, 1992) EC 3.2.1.-.
Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.
Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).
A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.
Chemical reaction in which monomeric components are combined to form POLYMERS (e.g., POLYMETHYLMETHACRYLATE).
Organic or inorganic compounds that contain the -N3 group.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Recording of pertinent information concerning patient's illness or illnesses.
Computer-based systems for input, storage, display, retrieval, and printing of information contained in a patient's medical record.
Media that facilitate transportability of pertinent information concerning patient's illness across varied providers and geographic locations. Some versions include direct linkages to online consumer health information that is relevant to the health conditions and treatments related to a specific patient.
The commitment in writing, as authentic evidence, of something having legal importance. The concept includes certificates of birth, death, etc., as well as hospital, medical, and other institutional records.
This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).
Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.
A management function in which standards and guidelines are developed for the development, maintenance, and handling of forms and records.

Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality. (1/87)

Caspases have been strongly implicated to play an essential role in apoptosis. A critical question regarding the role(s) of these proteases is whether selective inhibition of an effector caspase(s) will prevent cell death. We have identified potent and selective non-peptide inhibitors of the effector caspases 3 and 7. The inhibition of apoptosis and maintenance of cell functionality with a caspase 3/7-selective inhibitor is demonstrated for the first time, and suggests that targeting these two caspases alone is sufficient for blocking apoptosis. Furthermore, an x-ray co-crystal structure of the complex between recombinant human caspase 3 and an isatin sulfonamide inhibitor has been solved to 2.8-A resolution. In contrast to previously reported peptide-based caspase inhibitors, the isatin sulfonamides derive their selectivity for caspases 3 and 7 by interacting primarily with the S(2) subsite, and do not bind in the caspase primary aspartic acid binding pocket (S(1)). These inhibitors blocked apoptosis in murine bone marrow neutrophils and human chondrocytes. Furthermore, in camptothecin-induced chondrocyte apoptosis, cell functionality as measured by type II collagen promoter activity is maintained, an activity considered essential for cartilage homeostasis. These data suggest that inhibiting chondrocyte cell death with a caspase 3/7-selective inhibitor may provide a novel therapeutic approach for the prevention and treatment of osteoarthritis, or other disease states characterized by excessive apoptosis.  (+info)

Antagonism of adenosine 5'-triphosphate-induced relaxation by 2-2'-pyridylisatogen in the taenia of guinea-pig caecum. (2/87)

1. 2-2' Pyridylisatogen tosylate (PIT) (greater than 2.5 muM) relaxed the guinea-pig isolated taenia caeci by an unknown mechanism. 2. With higher concentrations of PIT (greater than 12.5 muM) subsequent applications of adenosine 5'-triphosphate (ATP) (2-600 muM) revealed a blockade of the ATP receptors. The antagonism was characterized by a delayed onset of action (greater than 10 min incubation with 50 muM PIT) and eventually became irreversible (greater than 50 muM PIT for greater than 30 minutes). The antagonism was specific for ATP, was not competitive, and was not dependent upon the relaxant effect. 3. The presence of either acetylcholine (0.05-1.0 muM) or carbachol (0.05-1.0 muM) increased the antagonistic effect of PIT (50 muM) approximately five-fold. 4. Following prolonged exposure, PIT (50 muM for 90 min) did not block the inhibitory effects of fiedl stimulation (2 Hz, 10 s) of the taenia caeci in the presence of hyoscine (0.33 muM). These results do not support the purinergic nerve hypothesis.  (+info)

Synthesis and pharmacological activities of hydrazones, Schiff and Mannich bases of isatin derivatives. (3/87)

Schiff bases and phenyl hydrazone of isatins were prepared by reacting isatin and the appropriate aromatic primary amine/hydrazines. A new series of the corresponding N-mannich bases were synthesized by reacting them with formaldehyde and diphenylamine. The chemical structures were confirmed by means of their 1H-NMR, IR spectral data and elemental analysis. The compounds were screened for analgesic, antiinflammatory and antipyretic activity. 1-Diphenylaminomethyl-3-(1-naphthylimino)-1,3-dihydroindol-3-one (4), 3-(1-naphthylimino)-5-bromo-1,3-dihydroindol-2-one (2) and 1-diphenylaminomethyl-3-(4-methylphenylimino)-1,3-dihydroindol-3-one (7) were found to exhibit the highest analgesic, anti-inflammatory and antipyretic activity respectively. 1-Diphenylaminomethyl-3-(4-methylphenylimino)-1,3-dihydroindol-3-one (7) was found to be the most active compound of the series.  (+info)

Characterization of a major form of human isatin reductase and the reduced metabolite. (4/87)

Isatin, an endogenous indole, has been shown to inhibit monoamine oxidase, and exhibit various pharmacological actions. However, the metabolism of isatin in humans remains unknown. We have found high isatin reductase activity in the 105,000 g supernatants of human liver and kidney homogenates, and have purified and characterized a major form of the enzyme in the two tissues. The hepatic and renal enzymes showed the same properties, including an M(r) of 31 kDa, substrate specificity for carbonyl compounds and inhibitor sensitivity, which were also identical to those of recombinant human carbonyl reductase. The identity of the isatin reductase with carbonyl reductase was immunologically demonstrated with an antibody against the recombinant carbonyl reductase. About 90% of the soluble isatin reductase activity in the liver and kidney was immunoprecipitated by the antibody. The Km (10 microm) and k(cat)/K(m) (1.7 s(-1) x microm(-1)) values for isatin at pH 7.0 were comparable to those for phenanthrenequinone, the best xenobiotic substrate of carbonyl reductase. The reduced product of isatin was chemically identified with 3-hydroxy-2-oxoindole, which is also excreted in human urine. The inhibitory potency of the reduced product for monoamine oxidase A and B was significantly lower than that of isatin. The results indicate that the novel metabolic pathway of isatin in humans is mediated mainly by carbonyl reductase, which may play a critical role in controlling the biological activity of isatin.  (+info)

The effects of isatin (indole-2, 3-dione) on pituitary adenylate cyclase-activating polypeptide-induced hyperthermia in rats. (5/87)

BACKGROUND: Previous studies have demonstrated that centrally administered natriuretic peptides and pituitary adenylate cyclase-activating polypeptide-38 (PACAP-38) have hyperthermic properties. Isatin (indole-2, 3-dione) is an endogenous indole that has previously been found to inhibit hyperthermic effects of natriuretic peptides. In this study the aim was to investigate the effects of isatin on thermoregulatory actions of PACAP-38, in rats. RESULTS: One microg intracerebroventricular (icv.) injection of PACAP-38 had hyperthermic effect in male, Wistar rats, with an onset of the effect at 2 h and a decline by the 6th h after administration. Intraperitoneal (ip.) injection of different doses of isatin (25-50 mg/kg) significantly decreased the hyperthermic effect of 1 microg PACAP-38 (icv.), whereas 12.5 mg/kg isatin (ip.) had no inhibiting effect. Isatin alone did not modify the body temperature of the animals. CONCLUSION: The mechanisms that participate in the mediation of the PACAP-38-induced hyperthermia may be modified by isatin. The capability of isatin to antagonize the hyperthermia induced by all members of the natriuretic peptide family and by PACAP-38 makes it unlikely to be acting directly on receptors for natriuretic peptides or on those for PACAP in these hyperthermic processes.  (+info)

Synthesis of isatin semicarbazones as novel anticonvulsants--role of hydrogen bonding. (6/87)

PURPOSE: A series of substituted isatin semicarbazones and related bioisosteric hydrazones were designed and synthesised to meet the structural requirements essential for anticonvulsant properties. METHODS: The structures of all synthesised compounds were confirmed by means of infrared, proton magnetic resonance spectroscopy and by elemental analyses. All compounds were evaluated for their anticonvulsant activity by maximal electroshock (MES), subcutaneous metrazol (ScMet) and subcutaneous strychnine (ScSty) induced seizure methods and their neurotoxic effects were determined by rotorod test. RESULTS: A number of isatin semicarbazones exhibited significant protection after intraperitoneal administration at the dose of 100 and 300mg/kg. Some of them showed good anticonvulsant activity in MES test in rats after per oral administration at the dose of 30mg/kg. The bioisosteric hydrazone derivatives were inactive in all tests. Compound 6-chloroisatin-3- (4-bromophenyl)-semicarbazone has emerged as the most active analogue of the series showing good activity in all the three tests and was more active than phenytoin and valproic acid. CONCLUSIONS: The results evidenced the importance of hydrogen bonding and suggested a new pharmacophore model with four binding sites essential for anticonvulsant activity.  (+info)

Investigating antibody-catalyzed ozone generation by human neutrophils. (7/87)

Recent studies have suggested that antibodies can catalyze the generation of previously unknown oxidants including dihydrogen trioxide (H(2)O(3)) and ozone (O(3)) from singlet oxygen ((1)O(2)(*)) and water. Given that neutrophils have the potential both to produce (1)O(2)(*) and to bind antibodies, we considered that these cells could be a biological source of O(3). We report here further analytical evidence that antibody-coated neutrophils, after activation, produce an oxidant with the chemical signature of O(3). This process is independent of surface antibody concentration down to 50% of the resting concentration, suggesting that surface IgG is highly efficient at intercepting the neutrophil-generated (1)O(2)(*). Vinylbenzoic acid, an orthogonal probe for ozone detection, is oxidized by activated neutrophils to 4-carboxybenzaldehyde in a manner analogous to that obtained for its oxidation by ozone in solution. This discovery of the production of such a powerful oxidant in a biological context raises questions about not only the capacity of O(3) to kill invading microorganisms but also its role in amplification of the inflammatory response by signaling and gene activation.  (+info)

Insights into the mode of inhibition of human mitochondrial monoamine oxidase B from high-resolution crystal structures. (8/87)

Monoamine oxidase B (MAO-B) is an outer mitochondrial membrane-bound enzyme that catalyzes the oxidative deamination of arylalkylamine neurotransmitters and has been a target for a number of clinically used drug inhibitors. The 1.7-A structure of the reversible isatin-MAO-B complex has been determined; it forms a basis for the interpretation of the enzyme's structure when bound to either reversible or irreversible inhibitors. 1,4-Diphenyl-2-butene is found to be a reversible MAO-B inhibitor, which occupies both the entrance and substrate cavity space in the enzyme. Comparison of these two structures identifies Ile-199 as a "gate" between the two cavities. Rotation of the side chain allows for either separation or fusion of the two cavities. Inhibition of the enzyme with N-(2-aminoethyl)-p-chlorobenzamide results in the formation of a covalent N(5) flavin adduct with the phenyl ring of the inhibitor occupying a position in the catalytic site overlapping that of isatin. Inhibition of MAO-B with the clinically used trans-2-phenylcyclopropylamine results in the formation of a covalent C(4a) flavin adduct with an opened cyclopropyl ring and the phenyl ring in a parallel orientation to the flavin. The peptide bond between the flavin-substituted Cys-397 and Tyr-398 is in a cis conformation, which allows the proper orientation of the phenolic ring of Tyr-398 in the active site. The flavin ring exists in a twisted nonplanar conformation, which is observed in the oxidized form as well as in both the N(5) and the C(4a) adducts. An immobile water molecule is H-bonded to Lys-296 and to the N(5) of the flavin as observed in other flavin-dependent amine oxidases. The active site cavities are highly apolar; however, hydrophilic areas exist near the flavin and direct the amine moiety of the substrate for binding and catalysis. Small conformational changes are observed on comparison of the different inhibitor-enzyme complexes. Future MAO-B drug design will need to consider "induced fit" contributions as an element in ligand-enzyme interactions.  (+info)

Muricid molluscs are a organic source of brominated isatin with anticancer activity. In conclusion this study supports 6-bromoisatin in Muricidae extracts as a promising lead for prevention of colorectal cancer. model, ocean mollusc 1. Intro Isatin BAX (1[6] demonstrated that isatin at a focus of 100 Meters decreased cell expansion of human being promyelocytic leukemia (HL60) tumor cells by 80% and caused morphological adjustments constant with proapoptotic cells (including DNA fragmentation and chromatin moisture build-up or condensation). In another scholarly research by Igosheva [7], apoptosis was observed in human neuroblastoma SH-SY5Y cells exposed to 50 M of isatin. A range of mono-substituted isatins have been studied by Vine [8] for their cytotoxicity on a lymphoma (U937) cell line. Structure activity relationship studies have shown that substitution with halogens (5-bromo-, 5-iodo-, and 5-fluoroisatin) yielded 5C10 times more activity for killing cancer cells, than the unsubstituted ...
|p|Oxidation of isatins (isatin, 5-methylisatin, 5-bromoisatin and 5-nitroisatin) to their anthranilic acids was performed efficiently with sodium N-chlorobenzenesulfonamide or chloramine-B (CAB) in alkaline medium at 35±0.1°C. The reactions follow identical kinetics for all the isatins, being first-order dependence each in [CAB]o and [Isatin]o and inverse fractional-order on [NaOH]. Addition of halide ions and benzenesulfonamide, reduction product of CAB, do not significantly affect the rate. Variation of ionic strength of the medium had no effect on the rate, while the dielectric effect is negative. The solvent isotope effect was studied using D2O. Activation parameters for the overall reaction have been computed. The rates satisfactorily correlate with the Hammett σ relationship and the reaction constant ρ is −0.31 signifies that electron releasing groups accelerate the reaction while the electron withdrawing groups retard the rate. Values of ΔH≠ and ΔS≠ are linearly
To develop more potent small molecules with enhanced free radical scavenger properties, a series of N-substituted isatin derivatives was synthesized, and the cytoprotective effect on the apoptosis of PC12 cells induced by H2O2 was screened. All these compounds were found to be active, and N-ethyl isatin was found with the most potent activity of 69.7% protective effect on PC12 cells. Structure-activity relationship analyses showed the bioactivity of N-alkyl isatins decline as the increasing of the chain of the alkyl group, furthermore odd-even effect was found in the activity, which is interesting for further investigation.
The report generally describes benz(f)isatin, examines its uses, production methods, patents. Benz(f)isatin market situation is overviewed; benz(f)isatin
Series of Novel isatinderivatives were investigated forinhibitionof HIVIntegrase/ Lens epithelium derived growth factor (LEDGF)protein-protein interaction by using ALPHA screen technique. Hypothetical binding modes of the selected compound in HIV integrase were generated using GLIDE docking tool.Isatin derivatives (SP III-5H and SPIII-NA) inhibits HIV IN/LEDGF interaction and SPIII-5H more potent compound (15.1 μM) in this series. Molecular modeling studies indicate that the SPIII-5H can bind within the active site of HIV integrase (DDE) and thus interrupt the binding of HIV integrase with LEDGF.
Chiral α-hydroxyamide L5 derived from (S)-(+)-mandelic acid catalyzes the enantioselective addition of dimethylzinc to isatins affording the corresponding chiral 3-hydroxy-3-methyl-2-oxindoles with good yields and er up to 90:10. Furthermore, several chemical transformations were performed with the 3-hydroxy-2-oxindoles obtained.
Indoles represent a structural element in a myriad of natural products and biologically active molecules. Of special importance are 2,3-disubstituted indoles. Thus, a number of methods for their synthesis have been described. However, these are often hampered by a number of limitations: they often offer poor regioselectivity and suboptimal functional group tolerance. Also, they can normally be adapted to the procurement of a small subclass of indoles only. We have developed an approach to 2,3-disubstituted indoles overcoming these obstacles. By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a regiospecific and functional group-tolerant manner. The methodology is normally characterized by excellent yields. The reaction proceeds by chemoselective partial reduction of the amide moiety to an iminium salt and a subsequent nucleophilic addition followed by dehydration, which furnishes the target indole. A number of nucleophiles, including
To expertise the students in the art of synthesizing various organic compounds by applying various organic reactions and thereby introducing the mechanism behind the reaction.
The development of a new polymerization methodology affords polymer materials with new structures and functionalities. Multicomponent polymerizations (MCPs) as a facile tool for preparing multifunctional polymers with complicated structures have attracted increasing attention from polymer scientists, owing t Emerging Investigators
TY - JOUR. T1 - Stereoselective three-component synthesis of trans-endo-decahydroquinolin- 4-one derivatives from aldehydes, aniline, and acetylcyclohexene. AU - Lin, Chunchi. AU - Fang, Hulin. AU - Tu, Zhijay. AU - Liu, Ju Tsung. AU - Yao, Ching Fa. PY - 2006/8/18. Y1 - 2006/8/18. N2 - The diastereoselective synthesis of trans-endo-decahydroquinolin-4-one (4) via a three-component reaction of aldehydes (1), anilines (2), and 1-acetylcyclohexene (3) in the presence of iodine in a one-pot reaction at room temperature is described. The short reaction time, easy workup, excellent yield, and mild reaction conditions make this novel annulation strategy both practical and attractive.. AB - The diastereoselective synthesis of trans-endo-decahydroquinolin-4-one (4) via a three-component reaction of aldehydes (1), anilines (2), and 1-acetylcyclohexene (3) in the presence of iodine in a one-pot reaction at room temperature is described. The short reaction time, easy workup, excellent yield, and mild ...
The interaction between isatin-β-thiosemicarbazone (IBT) and calf thymus DNA (CT-DNA) was investigated in physiological buffer (pH 7.4) using Neutral Red (NR) dye as a spectral probe by UV-Vis absorption and fluorescence spectroscopy, as well as viscosity measurements. The IBT is stabilized by intercalation in the DNA ( K [IBT -DNA] =1.03×105 M−1), and displaces the NR dye from the NR-DNA complex. The binding constants Kf and number of binding sites (n≈1) of IBT with DNA were obtained by fluorescence quenching method at different temperatures. Furthermore, the enthalpy and entropy of the reaction between IBT and CT-DNA showed that the reaction is enthalpy-favored and entropy-disfavored. The changes in the base stacking of CT-DNA upon the binding of IBT are reflected in the circular dichroic (CD) spectral studies. The viscosity increase of CT-DNA solution is another evidence to indicate that, IBT is able to be intercalated in the DNA base pairs.
Z)- N- (benzo[d]oxazol-2-yl)-2-(2-(2-oxoindolin-3- ylidene) hydrazineyl) ethanethioamide Compound VI a: Yellow Solid, 1H NMR (500 MHz, DMSO) δ 8.25 (s, 1H), 8.18 (dd, J = 8.8, 5.2 Hz, 3H), 8.09 (dd, J = 7.8, 6.4 Hz, 3H), 8.05 (s, 1H), 8.01 - 7.99 (m, 1H), 7.91 (d, J = 8.1 Hz, 2H), 7.72 - 7.69 (m, 1H), 7.67 (s, 1H), 7.58 (d, J = 5.5 Hz, 1H), 7.42 (d, J = 8.0 Hz, 1H), 7.33 - 7.27 (m, 3H), 6.96 (d, J = 7.0 Hz, 1H), 6.03 (s, 2H).13C NMR (125 MHz, DMSO) δ 188.00 (s), 140.78 (s), 139.48 (s), 138.21 (s), 136.76 (s), 134.18 (s), 133.82 (s), 132.96 (s), 132.63 (s), 131.15 (s), 130.89 (s), 129.18 (s), 128.73 (s), 128.16 (s), 127.35 (s), 127.14 (s), 126.64 (s), 126.32 (s), 126.03 (s), 125.26 (s), 123.57 (d), J = 18.0 Hz), 122.20 (s), 121.23 (s), 116.03 (s), 113.04 (s), 111.81 (s), 47.97 (s).. (Z)- N- (4- chlorobenzo [d] oxazol-2-yl)-2-(2-(2-oxoindolin- 3- ylidene) hydrazineyl) ethane-thioamide Compound VI b: Yellow Solid, 1H NMR (500 MHz, DMSO) δ 8.25 (s, 1H), 8.20 - 8.16 (m, 3H), 8.09 (dd, J = 7.8, 6.4 ...
Nitrogenous heterocyclic compounds, oxindoles especially isatins and related heterocyles have excellent antifungal, anti-inflammatory, antimicrobial and anticancer activities. Oxindoles keto lactams (1-3) were synthesized according to modified Sandmayer method and their N-acetylated compounds (4-6) gave diazo-biphenyls (7-10) through ring cleavage and consequent cyclization reaction. Bis-amide (11), and Schiff-base (12) were synthesized from oxindoles respectively. The investigation of cytotoxicity of the synthesized compounds was carried out against brine shrimp lethality bioassay. In our present investigation some of the synthesized compounds such as halogen substituted acetylisatins (4-6) and the ring extended diazo-biphenyls, (7-10) have been shown to exhibit strong cytotoxic effect.. Key words: diazo-biphenyls; oxindoles; cytotoxicity; brine shrimp. DOI: 10.3329/dujps.v9i1.7423. Dhaka Univ. J. Pharm. Sci. 9(1): 1-6, 2010 (June). ...
REFERENCES. Abel E. Behavioral effects of isatin on open field activity and immobility in the forced swim test in rats. Physiol Behav. 1995;57(3):611-3. [ Links ] Alexi T, Borlongan C, Faull R, Williams C, Clark R, Gluckman P, et al. Neuroprotective strategies for basal ganglia degeneration: Parkinsons and Huntingtons diseases. Prog Neurobiol. 2000;60(5):409-70. [ Links ] Ariza S, Rueda D, Rincón J, Linares E, Guerrero M. Efectos farmacológicos sobre el sistema nervioso central inducidos por cumarina aislada de Hygrophila tyttha Leonard. Vitae. 2007;14(2):51-8. [ Links ] Baltacioglu E, Akalin FA, Alver A, Deger O, Karabulut E. Protein carbonyl levels in serum and gingival crevicular fluid in patients with chronic periodontitis. Arch Oral Biol. 2008;53(8):716-22. [ Links ] Bishnoi M, Chopra K, Kulkarni S. Involvement of adenosinergic receptor system in an animal model of tardive dyskinesia and associated behavioural, biochemical and neurochemical changes. Eur J Pharmacol. 2006;552(1-3):55-66. ...
A novel strategy to obtain side chain modified poly(oxindole biphenylylene) (POXI) by photoinduced copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) click reaction is described. In the first step, an alkyne-functionalized poly(oxindolebiphenylylene) (POXI-alkyne) is synthesized by superacid-catalyzed condensation of isatin with aromatic hydrocarbons. Subsequently, poly(ethylene glycol) methyl ether (Me-PEG), 1-pyrenemethanol (Py-OH) and 1,3-dibromopropane (DBP) are functionalized by azide groups via simple nucleophilic substitution reaction. Visible-light-induced CuAAC reaction between POXI-alkyne and the corresponding azide functionalized click components employing dibenzoyldiethylgermane (DBDEG) as photoactivator resulted in the formation of POXI-PEG, POXI-Py and insoluble network, respectively. Successful modification of POXI was confirmed by the spectral, (1H NMR, FT-IR, Fluorescence), chromatographic (GPC) and thermal (DSC) investigations ...
The unexpectedly uncatalyzed reaction between 2-amino-4-arylimidazoles, aromatic aldehydes and Meldrums acid has selectively led to the corresponding Knoevenagel-Michael adducts containing a free amino group in the imidazole fragment. The adducts derived from Meldrums acid have been smoothly converted into 1,7-diaryl-3-amino-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-ones and 3-(2-amino-4-aryl-1H-imidazol-5-yl)-3-arylpropanoic acids. The interaction of 2-amino-4-arylimidazoles with aromatic aldehydes or isatins and acyclic methylene active compounds has led to the formation of pyrrolo[1,2-c]imidazole-6-carbonitriles, pyrrolo[1,2-small es, Cyrillic]imidazole-6-carboxylates and spiro[indoline-3,7-pyrrolo[1,2-c]imidazoles], which can be considered as the analogues of both 3,3-spirooxindole and 2-aminoimidazole marine sponge alkaloids.. ...
Condensation of aromatic aldehydes, malononitrile and thioglycolic acid gives 5-amino-3-oxo-7-substitutedphenyl-2-substitutedarylidene-2,3-dihydro-7H-[1,3]thiazolo[3,2-a] pyridine-6,8-dicarbonitrile 1a-e. This acts as key intermediate for two series of final compounds 4a-e and 7a-e. In the first route compounds 1a-e are refluxed with hydroxylamine hydrochloride to yield tricyclic compound 8-amino-3,6-bis(substitutedphenyl)-1,3,3a,9a-tetrahydro-6H-isoxazolo[3,4:4,5]-[1,3]thiazolo[3,2-a]pyridin-5,7-dicarbonitrile 2a-e. These when condensed with isatin give the corresponding Schiff bases 3a-e. Condensation of 3a-e with bromoethoxyphthalimide give the final products 8-[(1N-ethoxyphthalimido-2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]-3,6-bis(substitutedphenyl)-1,3,3a,9a-tetrahydro-6H-isoxazolo[3,4:4,5] [1,3]thiazolo-[3,2-a]-pyridine-5,7-dicarbonitrile 4a-e. In the second pathway NH2 group of compounds 1a-e is protected by bezoylation to furnish 5a-e. These ...
Larry L. Klein, Valentina Petukhova, Baojie Wan, Yuehong Wang, Bernard D. Santasiero, David C. Lankin, Guido F.Pauli, Scott G. Franzblau, A Novel Indigoid Anti-tuberculosis Agent, Bioorganic & Medicinal Chemistry Letters, 24 (1), 268-270 (2014); at UIC College of Pharmacy Larry L. Klein, Michael D. Tufano, Synthesis of Substituted Isatins, Tet. Letters, 54(8), 1008-1011 (2013); at UIC College of Pharmacy Larry L. Klein, Valentina Petukhova, Synthesis of Tri-functional Bis-azide Photoaffinity Probe, Syn. Com., 43(16), 2242-2245 (2013); at UIC College of Pharmacy DeGoey, David A.; Grampovnik, David; Chen, Hui-Ju; Flosi, William; Klein, Larry L; Dekhtyar, Tatyana; Stoll, Vincent; Mamo, Mulugeta; Molla, Akhter; Kempf, Dale. . P1-Substituted Symmetry-Based Human Immunodeficiency Virus Protease Inhibitors with Potent Antiviral Activity against Drug-Resistant Viruses, Journal of Medicinal Chemistry , 54 (20)7094-7104 (2011); at Abbott Labs. Larry L. Klein; J. T. Randolph, Non-HIV antiviral agents, ...
In this study, we developed an in vivo method to determine drug effects on oxidation-induced apoptosis in the zebrafish brain caused by treatment with l-hydroxyglutaric acid (LGA). We confirmed that LGA-induced apoptosis was caused by oxidation by examining the presence of an oxidative product, nitrotyrosine. Next, we examined the effects of 14 characterized neuroprotectants on LGA-treated zebrafish, including: d-methione (d-Met), Indole-3-carbinol, deferoxamine (DFO), dihydroxybenzoate (DHB), deprenyl, l-NAME (N(G)-nitro-l-arginine methyl ester), n-acetyl l-cysteine (l-NAC), 2-oxothiazolidine-4-carboxylate (OTC), lipoic acid, minocycline, isatin, cortisone, ascorbic acid and α-tocopherol. Eleven of 14 neuroprotectants and 7 of 7 synthetic anti-oxidants exhibit significant protection in zebrafish. Buthionine sulfoximine (BSO), used as a negative control, exhibited no significant protective effects. In addition, three blood-brain barrier (BBB) impermeable compounds exhibited no significant effects. Our
Diaz P, Xu J, Astruc-Diaz F, Pan HM, Brown DL, Naguib M (August 2008). Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective cannabinoid receptor 2 agonists for the treatment of neuropathic pain. Journal of Medicinal Chemistry. American Chemical Society. 51 (16): 4932-47. doi:10.1021/jm8002203. PMID 18666769 ...
Most of us would have tasted plums at some point or at least heard of it. They are a delicious addition to desserts. Also, cakes and pickles are made from it. Plums belong to the cherries and peaches family. There are over 2000 varieties of plums in the world. Did you know that globally plums are the 2nd most cultivated fruit? They are commercially cultivated on all the continents with the exception of Antarctica. Dried plums are also known as prunes. These fruits come in a gamut of colours and sizes. The usual colours are deep purple, reddish purple, red, green, white and yellow.. We take a look at some of the health benefits of plums.. Helps in Digestion. Plums are rich in isatine, sorbitol and dietary fibre. These elements get rid of digestive problems as well as constipation. Isanin and sorbitol possess laxative properties and stimulate fluid secretion in the bowels.. Staves off Diabetes. These fruits have a low glycemic index. So, eating them reduces the blood sugar and prevents the onset ...
A three-component reaction of an alpha ,alpha -disubstituted alpha -isocyanoacetamide, an aldehyde and an amino alc. afforded 5-iminooxazolines, which, upon sapon., cyclized under acidic conditions to provide the macrocyclodepsipeptides in good overall yields. [on SciFinder (R)]. Keywords: Alcohols Role: RCT (Reactant) ; RACT (Reactant or reagent) (amino; prepn. of iminooxazolines via ammonium chloride-promoted three-component reaction of isocyanoacetamides ; aldehydes and amino alcs.); Peptides Role: SPN (Synthetic preparation) ; PREP (Preparation) (depsipeptides ; macrocyclic; prepn. of macrocyclodepsipeptides via cyclization of iminooxazolines); Aldehydes Role: RCT (Reactant) ; RACT (Reactant or reagent) (prepn. of iminooxazolines via ammonium chloride-promoted three-component reaction of isocyanoacetamides ; aldehydes and amino alcs.); Ugi reaction (prepn. of isocyanoacetamides via Ugi reaction of ketones ; ammonium formate and isocyanoacetates); Ketones Role: RCT (Reactant) ; RACT (Reactant ...
A multicomponent reaction of indane-1,3-dione, an aldehyde and an amine-containing aromatic compound leading to the formation of indenopyridine-based heterocyclic medicinal scaffolds has been investigated. It was found that the yields significantly improve when oxygen gas is bubbled through the reaction mixt
IBT of Miamis parent company wins bid for hospital project in Spain. IBT of Miamis parent company, Eurofinsa, a global construction firm that specializes in public infrastructure, was awarded a joint-venture contract for the second phase of a $116 million hospital that will serve a population of 75,000 in northeastern... - PR12777424
Its been a while since Inclined Bed Therapy was introduced to this forum and thought it is a good time to ask for progress updates from those of us using IBT. A new page on Facebook has stimulated some very interesting results and I hear from new people testing IBT almost every day with the same predictable positive results. For those of you who have not yet heard about what IBT is and has already achieved for people with multiple sclerosis. Inclined Bed Therapy has been shown to
Many forms of solid tumor have a characteristic feature known as hypoxia, which describes a low or non-existent presence of oxygen in the cellular microenvironment. This decrease in oxygen causes activation of the hypoxia inducible factor (HIF) pathway, which activates the transcription of many genes that cause cell proliferation, metastasis, increased glycolysis and angiogenesis. Increased HIF expression has been linked with poor patient prognosis, increased malignancy, and therapeutic resistance. Previous work in our lab has identified 1 and 2 as inhibitors of the HIF pathway, specifically as disrupters of the p300-HIF-1α complex formation. A library of sulfonamide analogs has been designed and synthesized with the intent of examining the SAR of this series of compounds and improving potency and physicochemical properties as compared with lead compounds 1 and 2. At the end, we have achieved a thorough understanding of the structural features critical for future optimization work ...
Many forms of solid tumor have a characteristic feature known as hypoxia, which describes a low or non-existent presence of oxygen in the cellular microenvironment. This decrease in oxygen causes activation of the hypoxia inducible factor (HIF) pathway, which activates the transcription of many genes that cause cell proliferation, metastasis, increased glycolysis and angiogenesis. Increased HIF expression has been linked with poor patient prognosis, increased malignancy, and therapeutic resistance. Previous work in our lab has identified 1 and 2 as inhibitors of the HIF pathway, specifically as disrupters of the p300-HIF-1α complex formation. A library of sulfonamide analogs has been designed and synthesized with the intent of examining the SAR of this series of compounds and improving potency and physicochemical properties as compared with lead compounds 1 and 2. At the end, we have achieved a thorough understanding of the structural features critical for future optimization work ...
IBT Media, publisher of Newsweek and The International Business Times, has named Alvaro Palacios chief operating officer.. Palacios previously served as head of US operations for Televisa Publishing + Digital.. In related IBT Media news, the companys direct sales team will now report directly to CMO Mitchell Caplan. ...
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Exciting Medical Research and Discovery in Circulation and gravity dealing with subjects ranging from sap flow in tall trees to cerebrospinal fluid, lymphatic fluid and blood circulation. by Andrew K Fletcher
Sleeping Inclined To Restore and Support Your Health For Free. Fascinating Science, Discovery, History and Medical Research In Circulation And Posture, by Andrew K Fletcher
I started IBT several months before my first balloon angio and i noticed improvements in my night time bladder and very slight improvements in mobility - albeit varied so recently had another balloon angio due to restenosis my bed is ...
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20096-30-4 - SZRYAIYNNPFNLD-VKAVYKQESA-N - 1-Methyl-1H-indole-2,3-dione 3-((2-(hydroxy(oxido)amino)phenyl)hydrazone) - Similar structures search, synonyms, formulas, resource links, and other chemical information.
(3-Hydroxy-5-methyl-2-oxo-2,3-dihydro-1H-indole-3-carbonyl)-urea | C11H11N3O4 | CID 596040 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
4,5,6-trimethoxy-1-methyl-1H-indole-2,3-dione - chemical structural formula, chemical names, chemical properties, synthesis references
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7-Propyl-1H-indole-2,3-dione | C11H11NO2 | CID 583824 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
A Lewis base catalyzed ring expansion of isatin with 2, 2, 2-trifluorodiazoethane (CF3CHN2) is developed. It is characterized that the merge of tetramethylethylenediamine and CF3CHN2 generates reactive triazene intermediates, which construct substituted 3-hydroxy-4-(trifluoromethyl)quinolinones with high efficiency. Synthetic application of the procedure is broadened by 3-trifluormethylpyrazole fused 3-hydroxy-4-(trifluoromethyl)quinolinone synthesis ...
Neuronal ubiquitin C-terminal hydrolase (UCH-L1) has been linked to Parkinsons disease (PD), the progression of certain nonneuronal tumors, and neuropathic pain. Certain lung tumor-derived cell lines express UCH-L1 but it is not expressed in normal lung tissue, suggesting that this enzyme plays a role in tumor progression, either as a trigger or as a response. Small-molecule inhibitors of UCH-L1 would be helpful in distinguishing between these scenarios. By utilizing high-throughput screening (HTS) to find inhibitors and traditional medicinal chemistry to optimize their affinity and specificity, we have identified a class of isatin O-acyl oximes that selectively inhibit UCH-L1 as compared to its systemic isoform, UCH-L3. Three representatives of this class (30, 50, 51) have IC(50) values of 0.80-0.94 micro M for UCH-L1 and 17-25 micro M for UCH-L3. The K(i) of 30 toward UCH-L1 is 0.40 micro M and inhibition is reversible, competitive, and active site directed. Two isatin oxime inhibitors increased
The predatory marine gastropod Dicathais orbita has been the subject of a significant amount of biological and chemical research over the past five decades. Natural products research on D. orbita includes the isolation and identification of brominated indoles and choline esters as precursors of Tyrian purple, as well as the synthesis of structural analogues, bioactivity testing, biodistributional and biosynthetic studies. Here I also report on how well these compounds conform to Lipinskis rule of five for druglikeness and their predicted receptor binding and enzyme inhibitor activity. The composition of mycosporine-like amino acids, fatty acids and sterols has also been described in the egg masses of D. orbita. The combination of bioactive compounds produced by D. orbita is of interest for further studies in chemical ecology, as well as for future nutraceutical development. Biological insights into the life history of this species, as well as ongoing research on the gene expression, microbial symbionts
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Acetophenone and benzophenone propiophenone series,Anisole and phenol and thiophenol series,Aniline series,Benzaldehyde and benzaldehyde oxime and phenylpropionaldehyde and phenyl acetaldehydeseries,Benzene and biphenyl series,Benzoic acid and benzoyl chloride series,Benzonitrile and benzoylacetonitrile and Benzamide Thiobenzamide series,Benzotrifluoride series,Benzyl alcohol and benzyl halogen and phenethyl alcohol and Styrene,Benzylamine and phenylethylamine series,Boronic acid series,Cinnamic aldehyde and Cinnamic acid series,Indole and indanone,Isatin and benzene sulfonylchloride and benzoylformate series,Phenyl acetonitrile and Phenylacetic acid and phenylpropionic acid and benzoylacetate series,Phenyl isocyanate phenyl isothiocyanate series,Phenylhydrazine series,Phthalic acid and anhydride series,Other,,Aromsyn Co.,Ltd.
Acetophenone and benzophenone propiophenone series,Anisole and phenol and thiophenol series,Aniline series,Benzaldehyde and benzaldehyde oxime and phenylpropionaldehyde and phenyl acetaldehydeseries,Benzene and biphenyl series,Benzoic acid and benzoyl chloride series,Benzonitrile and benzoylacetonitrile and Benzamide Thiobenzamide series,Benzotrifluoride series,Benzyl alcohol and benzyl halogen and phenethyl alcohol and Styrene,Benzylamine and phenylethylamine series,Boronic acid series,Cinnamic aldehyde and Cinnamic acid series,Indole and indanone,Isatin and benzene sulfonylchloride and benzoylformate series,Phenyl acetonitrile and Phenylacetic acid and phenylpropionic acid and benzoylacetate series,Phenyl isocyanate phenyl isothiocyanate series,Phenylhydrazine series,Phthalic acid and anhydride series,Other,,Aromsyn Co.,Ltd.
A simple one-pot synthesis of indenopyrrolopyrimidines and indolopyrrolopyrimidines through the cyclocondensation reaction of 6-aminouracils and ninhydrin and/or isatin i..
Cytochrome P450cam (a camphor hydroxylase) isolated from soil bacterium Pseudomonas putida shows potent importance in environmental applications such as the degradation of chlorinated organic pollutants and insect control agents. Introducing such chemicals can be hazardous to the environment due to their lack of biodegradation. In this thesis, I have studied the role of several P450cam mutants in the oxidation of 3-chloroindole to isatin and the role of wild type P450cam in the dealkylation of 1,4-dibutoxybenzene, a potent feeding-deterrent against stored product pests. Mutant (E156G/V247F/V253G/F256S) was the most active in the conversion of 3-chloroindole by P450cam. We propose two mechanisms for the dechlorination of 3-chloroindole by P450cam. To investigate structure-activity patterns of 1,4-dialkoxybenzenes against beetles, the octanol-water partition coefficients of selected dialkoxybenzenes were investigated. Furthermore, P. putida strain ATCC17453 was able to metabolize ...
Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. NSC-117199 was identified as a porent inhibitor of the protein tyrosine phosphatase (PTPa) Shp2. A focused library of analogs incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
Exiguobacterium sp. RMA utilized 4-chloroindole as its sole source of carbon and energy. The effect of initial concentrations of substrate on the 4-chloroindole degradation was studied and observed that strain PMA was capable of degrading 4-chloroindole up to concentration of 0.5 mM. The degradation pathway of 4-chloroindole was studied for Exiguobacterium sp. PMA based on metabolites identified by gas chromatography-mass spectrometry. 4-Chloroindole was initially dehalogenated to indole that was further degraded via isatin, anthranilic acid, and salicylic acid. The potential of strain PMA to degrade 4-chloroindole in soil was monitored using soil microcosms, and it was observed that the cells of strain PMA efficiently degraded 4-chloroindole in the soil. The results of microcosm studies show that strain PMA may be used for bioremediation of 4-chloroindole-contaminated sites. This is the first report of the bacterial degradation of 4-chloroindole. (C) 2014 Elsevier B.V. All rights reserved ...
CAS NO:627877-90-1; Chemical name:1H-Indole-1,3-dicarboxylic acid, 2,3-dihydro-2-oxo-3-phenyl-, diphenylester, (3S)- ; physical and chemical property of 627877-90-1, 1H-Indole-1,3-dicarboxylic acid, 2,3-dihydro-2-oxo-3-phenyl-, diphenylester, (3S)- is provided by ChemNet.com
I have recommended IBT to all my MS patients. I shall let you have any feedback that I get. From What I read in this thread it appears to be useful in other conditions also. I have many ME/CFS patients ...
Boc Sciences offers cas 864754-32-5 1,2-Dimethyl-1H-indole-7-boronic acid in bulk,please inquire us to get a quote for 864754-32-5 1,2-Dimethyl-1H-indole-7-boronic acid.
The ORBITA trial published in Lancet showed that PCI did not increase exercise time or reduce angina by more than the effect of a sham procedure at 6 weeks on top of intensive medical therapy among 200 stable patients with single-vessel CAD. Although the media hype and editorial were misleading based on the very selected cohort that was randomized, it was a landmark study because it used a sham PCI procedure for the first time. ISCHEMIA is nearing 5,000 randomizations, and we need your help to reach and hopefully exceed this goal by the end of 2017. As you know, the ISCHEMIA primary endpoint is clinical events. Quality of life over time is a secondary endpoint. ORBITA supports equipoise for the management of SIHD and reinforces the importance of ISCHEMIA.. ...
The selective activity of genes is affected by displacements (morpho-genetic movements) of cells, their spatial location. They are provided by the ability of cells to actively move and adhere (selective formation of contacts with each other, in which glycocalyx plays an important role). Neighboring cells exert physical, chemical, and other influences on the cells that migrated and came into contact with them, selectively activating and inactivating the genes of their nuclei. Morphogenetic movement of cells is one of the mechanisms of selective activation of genes ...
TY - JOUR. T1 - Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N6-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists. AU - Nayak, Akshata. AU - Chandra, Girish. AU - Hwang, Inah. AU - Kim, Kyunglim. AU - Hou, Xiyan. AU - Kim, Hea Ok. AU - Sahu, Pramod K.. AU - Roy, Kuldeep K.. AU - Yoo, Jakyung. AU - Lee, Yoonji. AU - Cui, Minghua. AU - Choi, Sun. AU - Moss, Steven M.. AU - Phan, Khai. AU - Gao, Zhan Guo. AU - Ha, Hunjoo. AU - Jacobson, Kenneth A.. AU - Jeong, Lak Shin. PY - 2014/2/27. Y1 - 2014/2/27. N2 - Truncated N6-substituted-(N)-methanocarba-adenosine derivatives with 2-hexynyl substitution were synthesized to examine parallels with corresponding 4′-thioadenosines. Hydrophobic N6 and/or C2 substituents were tolerated in A3AR binding, but only an unsubstituted 6-amino group with a C2-hexynyl group promoted high hA 2AAR affinity. A small hydrophobic alkyl (4b and 4c) or N 6-cycloalkyl group (4d) ...
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5-((4-trifluoromethyl-biphenyl-2-carbonyl)-amino)-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide: structure in first source
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You are viewing an interactive 3D depiction of the molecule 4,6-dichloro-3-[(e)-(2-oxo-1-phenyl-3-pyrrolidinylidene)methyl]-1h-indole-2-carboxylic acid (C20H14Cl2N2O3) from the PQR.
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You are viewing an interactive 3D depiction of the molecule 6-[(carboxycarbonyl)amino]-1h-indole-5-carboxylic acid (C11H8N2O5) from the PQR.
28899-75-4 - NVKAHBFPKVINGE-UHFFFAOYSA-N - 7-Chloro-1H-indole-2-carboxylic acid - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Lookchem Provide Cas No.656237-91-1 Basic information: Properties,Safety Data,Sds and Other Datebase. We also Provide Trading Suppliers & Manufacture for 656237-91-1 1H-Indole-3-acetamide, 5,6-dihydroxy-alpha-oxo- (9CI).
1H-Indole-5-carboxylic acid, 3-[2-(dimethylamino)ethyl]-, ethyl ester. CAS 137499-21-9. Molecular Formula:C15H20N2O2. Molecular Weight:C15H20N2O2.
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A basic necessity, these entry-level winders are compact and lightweight. They are ideal for use in safes without the need for a plug-in adapter. Equipped with Orbita long-lived lithium D cell batteries operating on the 8-minute winding cycle, the batteries will last for many years without the need for replacement. Even longer life may be accomplished by using the 12-minute or extended-winding cycle, which is easily selected using the toggle switch located behind the mounting cup.. Product Dimensions: 4.2″H x 9.5″W x 5.8″L. ALL OUTLET STORE ITEMS ARE DISCOUNTED ACCORDINGLY DUE TO MINOR SURFACE IMPERFECTIONS. THE WINDERS ARE NEW AND FULLY GUARANTEED UNDER OUR 2-YEAR MANUFACTURERS WARRANTY. THERE ARE NO REFUNDS AVAILABLE FOR CLOSEOUT ITEMS.. ...
Using only urine (ammonia) and natural indigo, the sig vat is perhaps the least polluting, most environmentally-sound of all the indigo vat recipes, but the need to collect and store urine, the smell, and the need for multiple dips to obtain darker blues meant the dyeing industry welcomed development of new methods of dyeing with indigo. By the…
Abstract:. Chronic kidney disease appears worldwide. In the United States, the number of patients suffering from kid- ney failure doubled from 1998 to 2010. A common treat- ment for these patients is haemodialysis. However, the frequency of deaths caused by cardiovascular diseases is up to 10% to 30% higher in patients undergoing dialysis than in the general population. To analyse the underly- ing effects and for a possible risk prediction, a continuous monitoring of the ionic concentrations that are influenced by dialysis is desired. In this work, a method for the re- construction of the ionic concentrations of calcium and potassium from the ECG is proposed. In a first step, 91 monodomain simulations with the ten Tusscher ventricular cell model were performed for different extracellular ionic concentrations. From there, a standard 12-lead ECG was extracted. Calcium and potassium changes yielded ECGs clearly differing in amplitude and morphology. In a second step, the simulated ECG signals were ...
Notably, it is used to synthesize isatin. In this synthesis, chloral hydrate reacts with aniline and hydroxylamine to give a ... Marvel, C. S.; Hiers, G. S. (1941). "Isatin". Organic Syntheses.; Collective Volume, 1, p. 327 Chandrasekhar, S.; Shrinidhi, A ...
It was observed that isatin (an indole) forms a blue dye if it is mixed with sulfuric acid and crude benzene. The formation of ... Ward C., Sumpter (1944). "The Chemistry of Isatin". Chemical Reviews. 34 (3): 393-434. doi:10.1021/cr60109a003. Voosen, Paul ( ...
Stollé, R.; Bergdoll, R.; Luther, M.; Auerhahn, A.; Wacker, W. (1922). "Über N-substituierte Oxindole und Isatine". J. Prakt. ... Stollé, R.; Bergdoll, R.; Luther, M.; Auerhahn, A.; Wacker, W. (1930). "Über N-substituierte Oxindole und Isatine". J. Prakt. ... Sumpter, Ward C. (1944). "The Chemistry of Isatin". Chem. Rev. 34 (3): 393-434. doi:10.1021/cr60109a003. Sumpter, Ward C. (1945 ... Indole Hinsberg oxindole synthesis Stollé, R. (1913). "Über eine neue Methode zur Darstellung N-substituierter Isatine. ( ...
N-Oxy-isatin auso-Nitro-benzoylchlorid". Chem. Ber. 60 (6): 1364-1370. doi:10.1002/cber.19270600616.CS1 maint: multiple names: ...
Baum, H. M.; Sanders, R. G.; Straub, G. J. (1951). "The Occurrence of a Diphenyl Isatin in California Prunes". Journal of the ... In 1885, it was reported that condensation of isatin with phenol 2 leads to 3, which is Acetylated to (4). Oxyphenisatin has ... The ketone group of isatin (1) is nonenolizable and has interesting properties. In strong acid it becomes protonated, and the ... Baeyer, A.; Lazarus, M. J. (1885). "Ueber Condensationsproducte des Isatins". Berichte der Deutschen Chemischen Gesellschaft. ...
He also worked on the synthesis of isatin. and several reactions have been named after him: Sandmeyer isonitrosoacetanilide ... isatin synthesis(1919) and Sandmeyer diphenylurea isatin synthesis(1903). http://www.sciencephoto.com/media/228558/enlarge Hans ...
Indigo can be converted to isatin and then to oxindole. Then, in 1866, Adolf von Baeyer reduced oxindole to indole using zinc ...
It is a hydroxy derivative of oxindole first prepared by reducing isatin with sodium amalgam in an alkaline solution. Indole ... dioxindole converts to isatin through oxidation. The Martinet dioxindole synthesis is utilized in the preparation of oxindole ...
... and C6-substituted isatin analogues". Bioorg. Med. Chem. 19 (1): 261-74. doi:10.1016/j.bmc.2010.11.028. PMID 21134756. compound ... Chromone-3-phenylcarboxamides Isatins Phthalimides 8-Benzyloxycaffeines and CSC analogs (E,E)-8-(4-phenylbutadien-1-yl) ...
Bal TR, Anand B, Yogeeswari P, Sriram D (October 2005). "Synthesis and evaluation of anti-HIV activity of isatin beta- ...
Indoline Indole Indene Benzofuran Isoindoline Carboline Isatin Methylindole Carbazole Pyrrole Skatole Benzene Riggio, Oliviero ...
Another use is as a dissolved ozone indicator through the conversion to isatin-5-sulfonic acid. This reaction has been shown ... Kettle AJ, Clark BM, Winterbourn CC (April 2004). "Superoxide converts indigo carmine to isatin sulfonic acid: implications for ...
The reaction of isatin with a base such as potassium hydroxide hydrolyses the amide bond to give the keto-acid 2. This ... The Pfitzinger reaction (also known as the Pfitzinger-Borsche reaction) is the chemical reaction of isatin with base and a ... Reaction of N-acyl isatins with base gives 2-hydroxy-quinoline-4-carboxylic acids. Camps quinoline synthesis Friedländer ...
Synthesis of isatin via a process known as the Claisen isatin synthesis, described for the first time in 1879. Designer of a ...
4,7-Dihydroisoindole indole indene indoline benzofuran carbazole carboline isatin methylindole oxindole pyrrole skatole benzene ...
He described his first synthesis of indigo in 1878 (from isatin) and a second synthesis in 1880 (from 2-nitrobenzaldehyde). (It ...
In the Pfitzinger reaction of 1-tetralone with isatin, a compound called tetrofan (3,4-dihydro-1,2-benzacridine-5-carboxylic ...
... antifungal and anti-HIV evaluation of Schiff and Mannich bases of isatin derivatives with 3-amino-2-methylmercapto quinazolin-4 ...
Condensation with acenaphthoquinone gives 8, a dye of the so-called Ciba-Scarlet type, while condensation of 7 with isatin ...
"Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective cannabinoid receptor 2 ...
... an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins". Journal of Medicinal ...
... an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins". Journal of Medicinal ...
An ordinary bond of this type is only 148 pm and for comparison the C-C bond in isatin is 154 pm long. On the other hand, no ...
... isatin MeSH D03.438.473.600 - mazindol MeSH D03.438.473.615 - methisazone MeSH D03.438.473.629 - molindone MeSH D03.438.473.725 ...
... using anthranilic acid and ketones Pfitzinger reaction using an isatin with base and a carbonyl compound to yield substituted ...
... haberleri/fettah-tamince-sungate-port-royal-i-satin-aldi_25939.html Missing or empty ,title= (help) http://medya.haber3.com/ ...
Sakurai reaction Salol reaction Sandheimer Sandmeyer diphenylurea isatin synthesis Sandmeyer isonitrosoacetanilide isatin ...
... a chemical present in the browning reaction of fruits Isatin Phthalimide This set index page lists chemical structure articles ...
PYGM appears to interact with PRKAB2, WDYHV1, PYGL, PYGB, 5-aminoisatin, 5-nh2_caproyl-isatin, PHKG1, PPP1CA, PPP1R3A, DEGS1, ...
... a chemical reaction of an allylic ester with strong base Claisen isatin synthesis 5243 Clasien, a minor planet This ...
"Reaction of isatins with 6-amino uracils and isoxazoles: isatin ring-opening vs. annulations and regioselective synthesis of ... Isatin is a well-known natural product which can be found in plants of the genus Isatis, in Couroupita guianensis, and also in ... The isatin core is also responsible for the color of "Maya blue" and "Maya yellow" dyes. The Sandmeyer methodology is the ... The presence of an aromatic ring, a ketone and a γ-lactam moiety, gives to isatin the rare potential to be used as both an ...
Isatin 98%, ACROS Organics 100g; Glass bottle Chemicals:Organic Compounds:Organic oxygen compounds:Organooxygen compounds: ... isatin,indoline-2,3-dione,2,3-indolinedione,indole-2,3-dione,isatine,2,3-dioxoindoline,pseudoisatin,tribulin,isotin,isatic acid ... isatin,indoline-2,3-dione,2,3-indolinedione,indole-2,3-dione,isatine,2,3-dioxoindoline,pseudoisatin,tribulin,isotin,isatic acid ...
ISATIN. C8 H5 N O2. JXDYKVIHCLTXOP-UHFFFAOYSA-N. Ligand Interaction. ...
Hz, H5 of isatin), 6.96 (t, 2H, Hz, H6 of isatin), 7.14 (t, 2H, Hz, H7 of isatin), 7.34 (d, 2H, Hz, H4 of isatin), 10.55 (s, D2 ... H4 of isatin), 7.01 (t, 1H, J = 7.5 Hz, H5 of isatin), 7.41 (t, 1H, J = 7.5 Hz, H6 of isatin), 7.73 (d, 1H, J = 7.8 Hz, H7 of ... H5 of isatin), 7.41 (t, 1H, J = 7.8 Hz, H6 of isatin), 7.63 (d, 2H, J = 8.4 Hz, Ar-H), 7.85 (d, 1H, J = 7.5 Hz, H7 of isatin), ... H6 of isatin), 7.15 (t, 1H, J = 7.8 Hz, H7 of isatin), 7.37 (d, 1H, J = 7.5 Hz, H4 isatin), 9.55 (d, 1H, J = 14.0 Hz, D2O exch ...
... Hany S. Ibrahim,1 Soha R. Abdelhadi,1 and Hatem A. Abdel-Aziz ... T. A. F. M. Hassan, A. A. Kadi, and H. A. K. Abdel-Aziz, "Novel N, N′-Hydrazino-bis-isatin Derivatives with Selective Activity ... M. Verma, S. N. Pandeya, K. N. Singh, and J. P. Stables, "Anticonvulsant activity of Schiff bases of isatin derivatives," Acta ... K. M. Khan, M. Khan, M. Ali et al., "Synthesis of bis-Schiff bases of isatins and their antiglycation activity," Bioorganic & ...
Isatin; CAS No.: 91-56-5; Linear Formula: C8H5NO2; Empirical Formula: C8H5NO2; find related products, papers, technical ... Isatin derivatives (bis-Schiff base) are synthesized by the condensation of the natural or synthetic isatins with hydrazine. ... Isatin 97% Synonym: 2,3-. Dioxo-. 2,3-. dihydroindole, 2,3-Diketoindoline, 2,3-Dioxoindoline, 2,3-Indolinedione, o- ... Isatin undergoes Pd(II)-catalyzed C-H addition by direct sp2/sp3 C-H bond activation to form 3-substituted-3-hydroxy-2. - ...
Isatin in a dose of 3.12 mg/kg ip was found to block the development of PGE2-induced fever in mice, while in a dose of 12.5 mg/ ... In rats isatin in a dose of 12.5 mg/kg ip blocked fever initiation, and at 25.0 mg/kg ip attenuated existing PGE2-induced fever ... Isatin or an analogue was injected simultaneously with PGE2 and the development of fever was tested, or the test compound was ... and isatin analogues (5-methylisatin, 6-hydroxyisatin, 7-ethylisatin, N-acety- lisatin) were tested on prostaglandin E2 (PGE2)- ...
... mandelic acid catalyzes the enantioselective addition of dimethylzinc to isatins affording the corresponding chiral 3-hydroxy-3 ... Catalytic Enantioselective Addition of Me2Zn to Isatins. Carlos Vila * , Andrés del Campo. ... Vila, C.; del Campo, A.; Blay, G.; Pedro, J.R. Catalytic Enantioselective Addition of Me2Zn to Isatins. Catalysts 2017, 7, 387 ... Chiral α-hydroxyamide L5 derived from (S)-(+)-mandelic acid catalyzes the enantioselective addition of dimethylzinc to isatins ...
... isatin is used as a reactant for preparation of oxindole derivatives as TAk1 kinase inhibitors and of isatin thiosemicarbazones ...
... isatin, isatin analogues, isatin binding proteins, isatin targets, biological and pharmacological activity ... Isatin itself is an endogenous oxidized indole with a wide spectrum of behavioral and metabolic effects. It has a distinct and ... We consider here the most promising biological targets for various isatin analogues and/or metabolites, which are employed for ... It is also possible that the level of endogenous isatin may influence the in vivo pharmacological activity of compounds ...
Human Monoamine Oxidase B: I199F mutant in complex with isatin. *DOI: 10.2210/pdb2bk5/pdb ...
Oxindole; Isatin; 1H-Indole-2,3-dione. e-EROS Encyclopedia of Reagents for Organic Synthesis. . ...
New isatin-indole molecular hybrids 5a-n have been synthesized and characterized by various spectroscopic tools. The in vitro ... New isatin-indole molecular hybrids 5a-n have been synthesized and characterized by various spectroscopic tools. The in vitro ... Synthesis, Spectroscopic Characterization and Antimicrobial Potential of Certain New Isatin-Indole Molecular Hybrids. Reem I. ... Synthesis, Spectroscopic Characterization and Antimicrobial Potential of Certain New Isatin-Indole Molecular Hybrids. Molecules ...
... isatin, examines its uses, production methods, patents. Benz(f)isatin market situation is overviewed; benz(f)isatin ... Benz(f)isatin market forecast. 6. BENZ(F)ISATIN MARKET PRICES. 6.1. Benz(f)isatin prices in Europe. 6.2. Benz(f)isatin prices ... Benz(f)isatin prices in North America. 6.4. Benz(f)isatin prices in other regions. 7. BENZ(F)ISATIN END-USE SECTOR 7.1. Benz(f) ... Benz(f)isatin application spheres, downstream products. 3. BENZ(F)ISATIN MANUFACTURING METHODS. 4. BENZ(F)ISATIN PATENTS. ...
The linear ranges were over three orders of magnitude and the detection limits were 2.5 x 10(-8) mol L(-1) for isatin, 2.5 x 10 ... Determination of isatin and monoamine neurotransmitters in rat brain with liquid chromatography using palladium ... It was found that the CME exhibited efficiently electrocatalytic of isatin and showed high sensitivity and stability for ... The electrochemical behaviors of isatin, monoamine neurotransmitters and their metabolites at this CME were investigated by ...
A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory ... Keywords: α-glucosidase inhibitor; molecular docking; isatin; thiazole; diabetic α-glucosidase inhibitor; molecular docking; ... A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory ... Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase ...
Find manufacturers and suppliers for 4-Chloro-7-methoxy isatin, 60706-07-2. Synonyms: 4-Chloro-7-methoxy-1H-indole-2,3-dione; 4 ...
Isatin, for spectrophotometric det. of proline and thiophene, ≥99.0% C8H5NO2 ... we report the syntheses of enantiopure spirocyclohexaneoxindoles through domino Michael-Aldol reactions between isatin derived ... construction of multifunctionalized spirocyclohexaneoxindoles through organocatalytic Michael-Aldol cyclization of isatin ...
Schiff Base; Isatins; Amino Acids; Dibutyltin (IV) Complexes; Spectral Studies; Antimicrobial Activity ... Schiff base complexes derived from substituted isatin and amino acids. Natural Science, 4, 170-178. doi: 10.4236/ns.2012.43025 ... Schiff base complexes derived from substituted isatin and amino acids () ...
Structural modifications to the isatin scaffold afforded a total of 51 isatin-based analogues, 21 of which were new. ... 5,7-Dibromo-N-(p-methylbenzyl)-isatin (39) was the most active compound overall and exhibited an IC50 value of 490 nM against ... U937 and Jurkat leukemic cell lines, after 24 h. 5,7-Dibromo-N-(p-trifluoromethylbenzyl)isatin (54) was also of interest, ... Structural modifications to the isatin scaffold afforded a total of 51 isatin-based analogues, 21 of which were new. ...
Isatins can be synthesized from α-formyl amides in good yields via one-pot intramolecular cyclization-oxidation reaction in the ... First Report on the Synthesis of Isatins via Pyridinium Chlorochromate Catalyzed Intramolecular Cyclization Reactions. Qiming ...
Room temperature multicomponent polymerizations of alkynes, sulfonyl azides, and N-protected isatins toward oxindole-containing ... Room temperature multicomponent polymerizations of alkynes, sulfonyl azides, and N-protected isatins toward oxindole-containing ... and N-protected isatins are developed to afford oxindole-containing poly(N-acylsulfonamide)s with advanced properties. After ... applicability of a series of electron-rich or electron-deficient alkynes and alkyl group or aromatic group-substituted isatins ...
... benzimidazolone-isatin conjugates (7a-d), and in vitro evaluation of their antiproliferative activity towards two breast cancer ... herein we report the synthesis of two novel series of thiazolidinone-isatin conjugates (4a-n) and thiazolo[3,2-a] ... In connection with our research program on the development of new isatin-based anticancer candidates, ... In connection with our research program on the development of new isatin-based anticancer candidates, herein we report the ...
... with isatin-3-phenyl imine (I-3-Ph-I). The acid dissociation constant of the ligand and the... ... Isatin-3-phenyl imine equilibrium studies formation constants This is a preview of subscription content, log in to check access ... Potentiometric investigations have been carried out on binary chelates of Co(II), Ni(II), Cu(II) and Zn(II) with isatin-3- ... Formation constants of some bivalent 3d metal ion complexes with isatin-3-phenyl imine in aqueous dioxane. ...
Y . I W SULFANILAMIDE AND ISATIN ANALOGUES AMONG THE NITROGEN HETEROCYCLES PART I S u l f a n i l y l D e r i v a t i v e s o f ... THE SANDMEYER ISATIN SYNTHESIS APPLIED TO PYRIDINE AND QUINOLINE-AMINES. код для вставки. код для вставки на сайт или в блог. ... SULFANILAMIDE AND ISATIN ANALOGUES AMONG THE NITROGEN HETEROCYCLES. PART 1. SULFANILYL DERIVATIVES OF PYRIDINE AND QUINOLINE- ...
Sodium isatin-5-sulfonate, 5-Isatinsulfonic acid sodium salt, 2,3-Dioxo-5-indolinesulfonic acid sodium salt, molecular formula ... Currently there are no suppilers available for Sodium isatin-5-sulfonate.. Welcome to suggest suppliers to chemBlink. ...
By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a ... Regiospecific synthesis of 2,3-disubstituted indoles from isatins. Artur Ulikowski​1, Anna Jaromin2, Giorgia Brancolini3, Luca ... indoles, isatins, Schwartzs reagent. Copyright. © 2016 Ulikowski et al.. Licence. This is an open access article distributed ... By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a ...
In the search for better FAAH inhibitors with potent activity; based on our previous isatin based lead compound 8c, we designed ... Design, Synthesis and Biological Evaluation of Novel N-1 and C-3 Functionalized Isatin Derivatives as FAAH Inhibitors. Fatty ... and synthesized a series of structural analogs of 8c by varying the substitutions at both N-1 and C-3 of the isatin scaffold. ...
Conclusion: Indole and Isatin affected the expression of multiple genes in the yeast to hyphal signal transduction pathway in ... Conclusion: Indole and Isatin affected the expression of multiple genes in the yeast to hyphal signal transduction pathway in ... Modulation of Genes Involved in Yeast to Hyphal form Signal Transduction in Candida albicans by Indole and Isatin. Author(s): ... In conclusion both Isatin and Indole may represent potential anti-virulence agents against Candida albicans. Indole derivatives ...
We are Professional Manufacturer of Bulk Stock Isatin Cas 91 56 5 company, Factory & Exporters specialize in Bulk Stock Isatin ... Find Bulk Stock Isatin Cas 91 56 5 Manufacturers & Suppliers from China. ... Home > Tags > Bulk Stock Isatin Cas 91 56 5(Total 24 Products for Bulk Stock Isatin Cas 91 56 5) ... and service capabilities for Bulk Stock Isatin Cas 91 56 5 , Bulk Stock Isatin Cas 91-56-5 , Bulk Stock Inositol Cas 6917-35-7 ...
  • The Sandmeyer methodology is the oldest and straightforward way for the synthesis of isatin. (wikipedia.org)
  • The Stolle procedure is considered the best alternative to Sandmeyer methodology for the synthesis of both substituted and unsubstituted isatins. (wikipedia.org)
  • More recent approaches to the synthesis of N-substituted isatins involves the direct oxidation of commercially available, substituted indoles or oxindoles with different oxidizing agents such as TBHP, IBX-SO3K, tBuONO etc. (wikipedia.org)
  • Because of this unique reactivity, isatin is considered one of the most valuable building blocks in organic synthesis. (wikipedia.org)
  • Synthesis of bis-Schiff bases of isatins and their antiglycation activity," Bioorganic & Medicinal Chemistry , vol. 17, no. 22, pp. 7795-7801, 2009. (hindawi.com)
  • Attia, M.I. Synthesis, Spectroscopic Characterization and Antimicrobial Potential of Certain New Isatin-Indole Molecular Hybrids. (mdpi.com)
  • Synthesis of isatin derivatives by condensation reaction. (biomedcentral.com)
  • Design, Synthesis, Characterization and Biological Evaluation of Some Novel Isatin Derivatives as Antitubercular Agents. (1library.net)
  • Our present work reports synthesis of two Schiff bases L 1 , L 2 prepared by condensation of phenylhydrazine with isatin and 5-bromoisatin respectively, employing a method different from reported one. (tsijournals.com)
  • Therefore, based on the above facts, our interest in this field, the present work deals with the synthesis, characterization and biological evaluation of both Schiff base ligands derived from isatin and 5-bromoisatin with phenylhydrazine and mixed ligand complex of Ni (II) with these novel Schiff bases. (tsijournals.com)
  • Isatin also is a synthetically versatile substrate that can be used to prepare a large variety of heterocyclic compounds, such as indoles and quinolines, and as a raw material for drug synthesis. (openaccesspub.org)
  • In the view of this fact, we have planned the synthesis of some novel isatin analogue and screening them for analgesic-anti-inflammatory activity. (openaccesspub.org)
  • Synthesis, in vitro α-glucosidase inhibitory activity and docking studies of novel chromone-isatin derivatives. (bireme.br)
  • The group's latest publication concerning "Organocatalytic asymmetric aldol reaction of ketones with isatins:straightforward stereoselective synthesis of 3-alkyl-3-hydroxyindolin-2-ones" has been published in Tetrahedron. (ccnu.edu.cn)
  • Isatin imines including Schiff bases 1b and isatin hydrazones 2 , which are the product of condensation of amines or hydrazines with isatins 1a , respectively, are considered as a pharmacophore for diverse spectrum of biological activities [ 1 - 5 ] (Figure 1 ). (hindawi.com)
  • Moreover, bis-Schiff bases of isatins 4 represent significant antiglycation activity [ 11 ]. (hindawi.com)
  • Six new Schiff bases formed from the condensation reaction of S-benzyldithiocarbazate (SBDTC) and S-methyldithiocarbazate (SMDTC) with selected diketones containing isatin derivatives namely isatin, 5-fluroisatin, 5-chloroisatin, 5-bromoisatin and methylisatin have been synthesised. (upm.edu.my)
  • X-ray crystallographic study of SB5ClISA and SB5BrISA Schiff bases proved that the condensation reaction between S-benzyldithiocarbazate with the isatin derivatives occur at the carbonyl position number 3 in the isatin ring. (upm.edu.my)
  • Bidentate Isatin Schiff Base Ligands Oxovanadium (IV) Complexes', International Journal of Heterocyclic Chemistry , 2(3), pp. 52-61. (ac.ir)
  • Ghammamy, S. Bidentate Isatin Schiff Base Ligands Oxovanadium (IV) Complexes. (ac.ir)
  • We also have isolated a complex of Vanadium (III) with isatin schiff bases in the solid phase. (ac.ir)
  • These when condensed with isatin give the corresponding Schiff bases 3a-e . (niscair.res.in)
  • The effects of isatin (2,3-dioxo-indole) and isatin analogues (5-methylisatin, 6-hydroxyisatin, 7-ethylisatin, N-acety- lisatin) were tested on prostaglandin E2 (PGE2)-induced fever in mice and rats. (scirp.org)
  • G. Telegdy, A. Adamik and V. Glover, "Antipyretic Action of Isatin and Its Analogues in Mice and Rats," Neuroscience and Medicine , Vol. 2 No. 1, 2011, pp. 1-5. (scirp.org)
  • We consider here the most promising biological targets for various isatin analogues and/or metabolites, which are employed for the development of various groups of therapeutics. (dovepress.com)
  • Structural modifications to the isatin scaffold afforded a total of 51 isatin-based analogues, 21 of which were new. (edu.au)
  • Isatin is an endogenous compound which acts as a selective inhibitor of monoamine oxidase (MAO) B. In this study a range of isatin analogues were tested for their in vitro inhibition of human MAO A and B. Most of the analogues were less potent than isatin. (westminster.ac.uk)
  • It is also possible that the level of endogenous isatin may influence the in vivo pharmacological activity of compounds possessing the isatin moiety. (dovepress.com)
  • Vine, Kara Lea, An investigation into the cytotoxic properties of isatin-derived compounds: potential for use in targeted cancer therapy, Doctor of Philosophy thesis, School of Biological Sciences, University of Wollongong, 2007. (edu.au)
  • By selectively activating the amide carbonyl in isatin-derived oxindoles, we obtained a number of the title compounds in a regiospecific and functional group-tolerant manner. (peerj.com)
  • This study suggests that isatin Mannich bases P1-P3 are good candidate compounds especially for the development of new cholinesterase inhibitors since they were 2.2-5.9 times better inhibitors than clinically used drug Tacrine. (bartin.edu.tr)
  • N-alkylation and allylation reduces the lability of the isatin nucleus towards bases, while maintaining its typical reactivity.The N-substituted isatin have been frequently used as intermediates and synthetic precursors for the preparation of a wide variety of heterocyclic compounds. (amrita.edu)
  • The compounds present are the indigoids, including isatin and dehydroindigo. (sciencebase.com)
  • A quinine-derived thiourea organocatalyst promoted the highly enantioselective addition of naphthols and activated phenols to ketimines derived from isatins. (upv.es)
  • 5-(Trifluoromethoxy)isatin is used as a reactant for preparation of oxindole derivatives as TAk1 kinase inhibitors and of isatin thiosemicarbazones via condensation with thiosemicarbazones as herpes simplex virus (HSV) inhibitors. (alfa.com)
  • Crystal structure analyses of Co(II) and Ni(II) complexes showed that [Ni(SMISA)2]·MeCN and [Co(SMISA)2]·MeCN are six-coordinate and have a distorted octahedral structure with the ligands coordinated to the metal ions as uninegatively charged tridentate chelating agents via the azomethine nitrogen, thiolate sulphur atom and carbonylic oxygen atoms of the isatin moiety. (upm.edu.my)
  • Complexes of Mn (II), Co (II), Ni (II), Cu (II) and Zn (II) were synthesized using isatin and p-phenylenediamine ligands. (rjptonline.org)
  • The effects of isatin Mannich bases incorporating (1-[piperidin-1-yl (P1)/morpholin-4-yl (P2)/N-methylpiperazin-1-yl (P3)]methyl)-1H-indole-2,3-dione) moieties against human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoenzymes hCA I and hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes were evaluated. (bartin.edu.tr)
  • In vivo effects of isatin on certain enzymes, lipids & serotonergic system of rat brain. (bvsalud.org)
  • To date, only few articles concerning the ring expansion of isatin derivatives has been reported. (wikipedia.org)
  • The presence of an aromatic ring, a ketone and a γ-lactam moiety, gives to isatin the rare potential to be used as both an electrophile and a nucleophile: indeed, it undergoes an enormous number of reactions, such as N-substitutions, electrophilic aromatic substitution at positions C-5 and C-7 of the phenyl ring, nucleophilic additions onto the C-3 carbonyl group, chemoselective reductions, oxidations, ring-expansions and spiro-annulations. (wikipedia.org)
  • The N-functionalization of the isatin core can be readily obtained by the deprotonation of the amino moiety, forming the corresponding sodium or potassium salt, and subsequent addition of an electrophile (e.g. alkyl or acyl halides). (wikipedia.org)
  • based on our previous isatin based lead compound 8c, we designed and synthesized a series of structural analogs of 8c by varying the substitutions at both N-1 and C-3 of the isatin scaffold. (alliedacademies.org)
  • The first one is an acid-catalyzed one-pot multicomponent reaction involving isatins, aminouracils, and isooxazolones to form isoxazoquinolines, important scaffolds in medicinal chemistry. (wikipedia.org)
  • The oxidation of isatin using hydrogen peroxide or chromic anhydride yields isatoic anhydride, a compound widely used either in herbicide products and in medicinal chemistry. (wikipedia.org)
  • In present era, the biological and pharmaceutical properties, potential application of isatin(2,3-dihydro-2,3-dioxo-1H-indole) and its derivatives in medicinal chemistry have been dragged considerable attention[ 13 - 17 ]. (tsijournals.com)
  • Isatin and 5-halo derivatives has reacted to form the schiff's bases , mannich bases and friedal craft alkylation's to form C-C, C-N, C=N bonds. (openaccesspub.org)
  • In addition, the hydrazinolysis of 4a-d yielded 3-hydrazonoindolin-2-one ( 2 ) and 1,2-di(arylidene)hydrazines 6a-d instead of hydrazones 17a-d , while hydrazinolysis of isatin ketazine 5 gave the expected 3-hydrazonoindolin-2-one ( 2 ). (hindawi.com)
  • Isatin, an extract from Strobilanthes cusia (Nees) Kuntze, was the base for synthesizing derivatives that were screened for antibacterial activity against oilfield water-borne bacteria. (biomedcentral.com)
  • In this paper, we designed aminopyrimidinimino isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. (medicinalchemistryinfo.com)
  • Isatin aldazines 4 showed a significant anticancer activity against human breast cell line MCF-7 [ 9 ], whereas a series of symmetrical and asymmetrical isatin ketazines 5 showed a selective activity against multidrug-resistant cancer cells [ 10 ]. (hindawi.com)
  • is a fluorinated isatin derivative that has been approved by FDA as a new anticancer drug to treat advanced renal carcinoma [9] and gastrointestinal stromal tumors [10]. (web-succes.com)
  • A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory activity. (mdpi.com)
  • The isatin derivatives were synthesized as shown in Scheme 1 . (biomedcentral.com)
  • In light of the latter results and in continuation of our interest in the chemistry of isatin-based azines 4 and 5 , we hope to report herein the unexpected results of hydrolysis and hydrazinolysis of isatin aldazines 4a-d and isatin ketazines 5 . (hindawi.com)
  • Isolation of this intermediate and subsequent electrophilic cyclization promoted by strong acids (e.g. sulfuric acid) furnishes isatin in >75% yield. (wikipedia.org)
  • Enantioselective construction of multifunctionalized spirocyclohexaneoxindoles through organocatalytic Michael-Aldol cyclization of isatin derived alkenes with linear dialdehydes. (sigmaaldrich.com)
  • Isatins can be synthesized from α-formyl amides in good yields via one-pot intramolecular cyclization-oxidation reaction in the presence of pyridinium chlorochromate (PCC). (organic-chemistry.org)
  • Isatin, also known as tribulin, is an organic compound derived from indole with formula C8H5NO2. (wikipedia.org)
  • Isatin itself is an endogenous oxidized indole with a wide spectrum of behavioral and metabolic effects. (dovepress.com)
  • New isatin-indole molecular hybrids 5a - n have been synthesized and characterized by various spectroscopic tools. (mdpi.com)
  • We have tried to identify potential targets of Indole and Isatin in the Yeast to hyphal induction signal transduction pathways in the human pathogen Candida albicans. (eurekaselect.com)
  • Objective: To study changes in gene expression during yeast to hyphal transition in the presence and absence of Indole and Isatin. (eurekaselect.com)
  • Results: The genes involved in Yeast to hyphal transition were modulated by the treatment of Indole and Isatin. (eurekaselect.com)
  • Our results indicate that Indole and Isatin may target multiple steps in the yeast to hyphal signal transduction pathway. (eurekaselect.com)
  • Hyphal suppressor genes Nrg1, Tup1 were significantly upregulated by Indole and Isatin. (eurekaselect.com)
  • Conclusion: Indole and Isatin affected the expression of multiple genes in the yeast to hyphal signal transduction pathway in Candida albicans. (eurekaselect.com)
  • In conclusion both Isatin and Indole may represent potential anti-virulence agents against Candida albicans. (eurekaselect.com)
  • Isatin or 1H-indole-2,3-dione is an indole derivative. (amrita.edu)
  • Isatin (1H-indole-2,3-dione ) and derivatives demonstrate a diverse array of biological activities. (openaccesspub.org)
  • Herein, we report the syntheses of enantiopure spirocyclohexaneoxindoles through domino Michael-Aldol reactions between isatin derived alkenes and pentane-1,5-dial in the presence of diphenylprolinol silyl ether as an aminocatalyst. (sigmaaldrich.com)
  • The three components coupling reactions of isatin, malononitrile and enolizable 4-hydroxycoumarin were performed in water as a green solvent. (ajgreenchem.com)
  • Chiral α-hydroxyamide L5 derived from ( S )-(+)-mandelic acid catalyzes the enantioselective addition of dimethylzinc to isatins affording the corresponding chiral 3-hydroxy-3-methyl-2-oxindoles with good yields and er up to 90:10. (mdpi.com)
  • From the spectral studies, isatin has undergoes reaction at C-3 and N-1 position and synthesized lead in present schme and seen the similarity of structure and analgesic-anti-inflammatory activity. (openaccesspub.org)
  • Isatin or an analogue was injected simultaneously with PGE2 and the development of fever was tested, or the test compound was given 30 min following PGE2 administration and the effects on the already existing fever were measured, in mice and in rats. (scirp.org)
  • In rats isatin in a dose of 12.5 mg/kg ip blocked fever initiation, and at 25.0 mg/kg ip attenuated existing PGE2-induced fever. (scirp.org)
  • Combined with microdialysis, the method was successfully applied to study the effect of isatin on the levels of monoamine neurotransmitters in experimental Parkinsonian rats. (nih.gov)
  • Administration of isatin to rats at 300 mg/kg body weight for 2 and 6 h significantly raised brain serotonin levels. (bvsalud.org)
  • Groothandel Organische Chemische Isatin Cas 91 56 5 met een hoge kwaliteit als een lage prijs / goedkoop, een van de toonaangevende merken van Organische Chemische Isatin Cas 91 56 5 uit China, Shenyu Energy (Shandong) Development Co. Ltd. (zgshenyu.com)
  • Dimerization of isatin with KBH4 in methanol yield Indirubin. (wikipedia.org)
  • Isatin (1 mmol) was dissolved in methanol (20 ml) and a methanol solution of 1.2 mmol amino compound (10 ml) was added dropwise, until the disappearance of isatin, as evidenced by thin-layer chromatography. (biomedcentral.com)
  • 2. In the fumehood , measure out 0.5g isatin powder and add to the methanol/acetic acid, then mix until fully dissolved with a stir rod. (ubc.ca)
  • A range of mono-substituted isatins have been studied by Vine [8] for their cytotoxicity on a lymphoma (U937) cell line. (web-succes.com)
  • Isatinic acid, which is formed reversibly from isatin at alkaline pH, showed no inhibition. (westminster.ac.uk)
  • Potentiometric investigations have been carried out on binary chelates of Co(II), Ni(II), Cu(II) and Zn(II) with isatin-3-phenyl imine (I-3-Ph-I). The acid dissociation constant of the ligand and the formation constants of its metal complexes have been determined at 30°C, in 10% volume of dioxane-water at ionic strengths of 0.1 M, 0.15 M, 0.1 M and 0.05 M KNO 3 . (springer.com)
  • After standing for about one-half hour, the isatin is filtered with suction, washed several times with cold water to remove the sulfuric acid , and then dried in the air. (orgsyn.org)
  • Determination of isatin and monoamine neurotransmitters in rat brain with liquid chromatography using palladium hexacyanoferrate modified electrode. (nih.gov)
  • The electrochemical behaviors of isatin, monoamine neurotransmitters and their metabolites at this CME were investigated by cyclic voltammetry. (nih.gov)
  • It was found that the CME exhibited efficiently electrocatalytic of isatin and showed high sensitivity and stability for determination of monoamine neurotransmitters. (nih.gov)
  • The results showed that isatin could significantly increase striatal monoamine neurotransmitters release to the basal level. (nih.gov)
  • Isatin (10 microM) strongly inhibited the activity of rat brain monoamine oxidase -B ( MAO-B ) in vitro . (bvsalud.org)
  • Isatin and its metabolites are constituents of many natural substances. (dovepress.com)
  • In another one-pot multicomponent reaction, a unique two-carbon expansion has been achieved by reacting isatin with indene-1,3-dione and N-substituted pyridinium bromide to form dibenzo[b,d]azepin-6-ones. (wikipedia.org)
  • In this work, a series of efficient one-pot multicomponent polymerizations of diynes, disulfonyl azides, and N -protected isatins are developed to afford oxindole-containing poly( N -acylsulfonamide)s with advanced properties. (rsc.org)
  • This MCP enjoys general applicability of a series of electron-rich or electron-deficient alkynes and alkyl group or aromatic group-substituted isatins, generating six poly( N -acylsulfonamide)s from different combination of monomers, and nitrogen gas as the only byproduct, demonstrating high atom economy and environmental benefit. (rsc.org)
  • 5,7-Dibromo-N-(p-methylbenzyl)-isatin (39) was the most active compound overall and exhibited an IC50 value of 490 nM against U937 and Jurkat leukemic cell lines, after 24 h. 5,7-Dibromo-N-(p-trifluoromethylbenzyl)isatin (54) was also of interest, considering the potent cell killing ability displayed against a metastatic breast adenocarcinoma (MDA-MB-231) cell line. (edu.au)
  • Hypothetical binding modes of the selected compound in HIV integrase were generated using GLIDE docking tool.Isatin derivatives (SP III-5H and SPIII-NA) inhibits HIV IN/LEDGF interaction and SPIII-5H more potent compound (15.1 μM) in this series. (semanticscholar.org)
  • Currently there are no suppilers available for Sodium isatin-5-sulfonate. (chemblink.com)
  • A novel series of chromone-isatin derivatives 6a-6p were designed, synthesized and characterized by H NMR, C NMR and HRMS. (bireme.br)
  • T. A. F. M. Hassan, A. A. Kadi, and H. A. K. Abdel-Aziz, "Novel N, N′-Hydrazino-bis-isatin Derivatives with Selective Activity against Multidrug-Resistant Cancer Cells," US Patents, US20120252860, 2012. (hindawi.com)
  • Structure activity relationship studies have shown that substitution with halogens (5-bromo-, 5-iodo-, and 5-fluoroisatin) yielded 5C10 times more activity for killing cancer cells, than the unsubstituted isatin [8]. (web-succes.com)
  • Isatin is a versatile compound isolated in 1988 and reported to possess a wide range of biological activity in mammals. (openaccesspub.org)
  • Recently, isatin is considered interesting heterocyclic compound due to its wide range of biological activities. (tsijournals.com)
  • Benz(f)isatin (CAS 5810-96-8) Market Research Report 2018 contents were prepared and placed on the website in February, 2018. (marketpublishers.com)
  • Please note that Benz(f)isatin (CAS 5810-96-8) Market Research Report 2018 is a half ready publication and contents are subject to change. (marketpublishers.com)
  • Study on the Interaction between Isatin-β-Thiosemicarbazone and Calf Thymus DNA by Spectroscopic Techniques', Iranian Journal of Pharmaceutical Research , 14(1), pp. 111-123. (ac.ir)
  • The interaction between isatin-β-thiosemicarbazone (IBT) and calf thymus DNA (CT-DNA) was investigated in physiological buffer (pH 7.4) using Neutral Red (NR) dye as a spectral probe by UV-Vis absorption and fluorescence spectroscopy, as well as viscosity measurements. (ac.ir)
  • However, isatin did not affect these enzymes after both acute and chronic treatments in vivo. (bvsalud.org)