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.
Group of alkaloids containing a benzylpyrrole group (derived from TRYPTOPHAN)
Compounds formed by condensation of secologanin with tryptamine resulting in a tetrahydro-beta-carboline which is processed further to a number of bioactive compounds. These are especially found in plants of the APOCYNACEAE; LOGANIACEAE; and RUBIACEAE families.
An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.
A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles.
A plant genus of the family Apocynaceae. It is the source of VINCA ALKALOIDS, used in leukemia chemotherapy.
An enzyme that catalyzes the conversion of L-tryptophan and water to indole, pyruvate, and ammonia. It is a pyridoxal-phosphate protein, requiring K+. It also catalyzes 2,3-elimination and beta-replacement reactions of some indole-substituted tryptophan analogs of L-cysteine, L-serine, and other 3-substituted amino acids. (From Enzyme Nomenclature, 1992) EC
An enzyme that catalyzes the conversion of L-serine and 1-(indol-3-yl)glycerol 3-phosphate to L-tryptophan and glyceraldehyde 3-phosphate. It is a pyridoxal phosphate protein that also catalyzes the conversion of serine and indole into tryptophan and water and of indoleglycerol phosphate into indole and glyceraldehyde phosphate. (From Enzyme Nomenclature, 1992) EC
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Indolesulfonic acid used as a dye in renal function testing for the detection of nitrates and chlorates, and in the testing of milk.
Substituted thioglucosides. They are found in rapeseed (Brassica campestris) products and related cruciferae. They are metabolized to a variety of toxic products which are most likely the cause of hepatocytic necrosis in animals and humans.
Alkaloid isolated from seeds of Peganum harmala L., Zygophyllaceae. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic Parkinson disease in the 1920's.
A plant genus of the APOCYNACEAE or dogbane family. Alkaloids from plants in this genus have been used as tranquilizers and antihypertensive agents. RESERPINE is derived from R. serpentina.
A plant genus of the family APOCYNACEAE. It contains ellipticine.
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.
Decarboxylated monoamine derivatives of TRYPTOPHAN.
The Madder plant family of the order Rubiales, subclass Asteridae, class Magnoliopsida includes important medicinal plants that provide QUININE; IPECAC; and COFFEE. They have opposite leaves and interpetiolar stipules.
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.
A group of indole-indoline dimers which are ALKALOIDS obtained from the VINCA genus of plants. They inhibit polymerization of TUBULIN into MICROTUBULES thus blocking spindle formation and arresting cells in METAPHASE. They are some of the most useful ANTINEOPLASTIC AGENTS.
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)
Acetic acid derivatives of the heterocyclic compound indole. (Merck Index, 11th ed)
Attachment of isoprenoids (TERPENES) to other compounds, especially PROTEINS and FLAVONOIDS.
Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
A plant family of the order Theales.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
Benzoic acids, salts, or esters that contain an amino group attached to carbon number 2 or 6 of the benzene ring structure.
An enzyme that, in the pathway of cholesterol biosynthesis, catalyzes the condensation of isopentenyl pyrophosphate and dimethylallylpyrophosphate to yield pyrophosphate and geranylpyrophosphate. The enzyme then catalyzes the condensation of the latter compound with another molecule of isopentenyl pyrophosphate to yield pyrophosphate and farnesylpyrophosphate. EC
An enzyme that catalyzes the chlorination of a range of organic molecules, forming stable carbon-chloride bonds. EC
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.
A plant genus of the family APOCYNACEAE. Members contain echitovenidine, echitamine, venenatine (an indole alkaloid), and anti-inflammatory triterpenoids
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
Compounds with a core of 10 carbons generally formed via the mevalonate pathway from the combination of 3,3-dimethylallyl pyrophosphate and isopentenyl pyrophosphate. They are cyclized and oxidized in a variety of ways. Due to the low molecular weight many of them exist in the form of essential oils (OILS, VOLATILE).
Inorganic or organic compounds derived from phosphine (PH3) by the replacement of H atoms. (From Grant & Hackh's Chemical Dictionary, 5th ed)
Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)
Any chemical species which accepts an electron-pair from a LEWIS BASE in a chemical bonding reaction.
A biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.
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.
A N-hydroxylated derivative of 2-ACETYLAMINOFLUORENE that has demonstrated carcinogenic action.
Toxins isolated from any species of the seaweed Lyngbya or similar chemicals from other sources, including mollusks and micro-organisms. These have been found to be potent tumor promoters. They are biosynthesized from TRYPTOPHAN; VALINE; and METHIONINE nonribosomally (PEPTIDE BIOSYNTHESIS, NUCLEIC ACID-INDEPENDENT).
Covalent attachment of HALOGENS to other compounds.
The immediate precursor in the biosynthesis of SEROTONIN from tryptophan. It is used as an antiepileptic and antidepressant.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Rhodium. A hard and rare metal of the platinum group, atomic number 45, atomic weight 102.905, symbol Rh. (Dorland, 28th ed)
A substance occurring in the urine of mammals and also in blood plasma as the normal metabolite of tryptophan. An increased urinary excretion of indican is seen in Hartnup disease from the bacterial degradation of unabsorbed tryptophan.
A plant genus of the family APOCYNACEAE that contains bisindole alkaloids and IBOGAINE.
Substances used for the detection, identification, analysis, etc. of chemical, biological, or pathologic processes or conditions. Indicators are substances that change in physical appearance, e.g., color, at or approaching the endpoint of a chemical titration, e.g., on the passage between acidity and alkalinity. Reagents are substances used for the detection or determination of another substance by chemical or microscopical means, especially analysis. Types of reagents are precipitants, solvents, oxidizers, reducers, fluxes, and colorimetric reagents. (From Grant & Hackh's Chemical Dictionary, 5th ed, p301, p499)
Compounds used extensively as acetylation, oxidation and dehydrating agents and in the modification of proteins and enzymes.
Chemical agents that increase the rate of genetic mutation by interfering with the function of nucleic acids. A clastogen is a specific mutagen that causes breaks in chromosomes.
A subclass of iridoid compounds that include a glucoside moiety, usually found at the C-1 position.
Techniques used in studying bacteria.
Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A plant genus of the family RUBIACEAE. Members contain uncarine and other cytotoxic and hypotensive oxindole alkaloids.
One of several indole alkaloids extracted from Tabernanthe iboga, Baill. It has a complex pharmacological profile, and interacts with multiple systems of neurotransmission. Ibogaine has psychoactive properties and appears to modulate tolerance to opiates.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
Measurement of the intensity and quality of fluorescence.
A family of gram-negative, facultatively anaerobic, rod-shaped bacteria that do not form endospores. Its organisms are distributed worldwide with some being saprophytes and others being plant and animal parasites. Many species are of considerable economic importance due to their pathogenic effects on agriculture and livestock.
The reaction of two molecular entities via oxidation usually catalyzed by a transition metal compound and involving dioxygen as the oxidant.
The dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters. Asclepiadacea (formerly the milkweed family) has been included since 1999 and before 1810.
Compounds in which a methyl group is attached to the cyano moiety.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A class of compounds composed of repeating 5-carbon units of HEMITERPENES.
Alkaloids extracted from various species of Cinchona.
Any liquid or solid preparation made specifically for the growth, storage, or transport of microorganisms or other types of cells. The variety of media that exist allow for the culturing of specific microorganisms and cell types, such as differential media, selective media, test media, and defined media. Solid media consist of liquid media that have been solidified with an agent such as AGAR or GELATIN.
Any salt or ester of glycerophosphoric acid.
A family of isomeric, colorless aromatic hydrocarbon liquids, that contain the general formula C6H4(CH3)2. They are produced by the destructive distillation of coal or by the catalytic reforming of petroleum naphthenic fractions. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Polymers where the main polymer chain comprises recurring amide groups. These compounds are generally formed from combinations of diamines, diacids, and amino acids and yield fibers, sheeting, or extruded forms used in textiles, gels, filters, sutures, contact lenses, and other biomaterials.
A genus of GRAM-POSITIVE ENDOSPORE-FORMING RODS in the family Paenibacillaceae.
A plant genus of the family Cruciferae. It contains many species and cultivars used as food including cabbage, cauliflower, broccoli, Brussel sprouts, kale, collard greens, MUSTARD PLANT; (B. alba, B. junica, and B. nigra), turnips (BRASSICA NAPUS) and rapeseed (BRASSICA RAPA).
A plant genus of the family RUBIACEAE. Members contain psychotridine and brachycerine (indole alkaloids).
Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.
Widely distributed enzymes that carry out oxidation-reduction reactions in which one atom of the oxygen molecule is incorporated into the organic substrate; the other oxygen atom is reduced and combined with hydrogen ions to form water. They are also known as monooxygenases or hydroxylases. These reactions require two substrates as reductants for each of the two oxygen atoms. There are different classes of monooxygenases depending on the type of hydrogen-providing cosubstrate (COENZYMES) required in the mixed-function oxidation.
The five-carbon building blocks of TERPENES that derive from MEVALONIC ACID or deoxyxylulose phosphate.
A type of MONOTERPENES, derived from geraniol. They have the general form of cyclopentanopyran, but in some cases, one of the rings is broken as in the case of secoiridoid. They are different from the similarly named iridals (TRITERPENES).
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
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.
Cyclic esters of acylated BUTYRIC ACID containing four carbons in the ring.
A plant genus of the family BRASSICACEAE that is an ingredient of the preparation PC-SPES that is used to treat PROSTATIC HYPERPLASIA.
Placing of a hydroxyl group on a compound in a position where one did not exist before. (Stedman, 26th ed)
Organic compounds containing carbon and hydrogen in the form of an unsaturated, usually hexagonal ring structure. The compounds can be single ring, or double, triple, or multiple fused rings.
A genus of gram-negative, facultatively anaerobic, rod-shaped bacteria whose organisms occur in the lower part of the intestine of warm-blooded animals. The species are either nonpathogenic or opportunistic pathogens.
The rate dynamics in chemical or physical systems.
A group of alicyclic hydrocarbons with the general formula R-C5H9.
A technology, in which sets of reactions for solution or solid-phase synthesis, is used to create molecular libraries for analysis of compounds on a large scale.
The study of the structure, preparation, properties, and reactions of carbon compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A genus of root and butt rot fungi in the family Tricholomataceae that produce rhizomorphs and are facultatively parasitic. Many species are pathogenic to trees causing Armillaria root disease.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
Any of the hormones produced naturally in plants and active in controlling growth and other functions. There are three primary classes: auxins, cytokinins, and gibberellins.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
The characteristic three-dimensional shape of a molecule.
A group of compounds derived from ammonia by substituting organic radicals for the hydrogens. (From Grant & Hackh's Chemical Dictionary, 5th ed)
Enzymes that hydrolyze O-glucosyl-compounds. (Enzyme Nomenclature, 1992) EC 3.2.1.-.
A phenomenon where microorganisms communicate and coordinate their behavior by the accumulation of signaling molecules. A reaction occurs when a substance accumulates to a sufficient concentration. This is most commonly seen in bacteria.
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
A genus of gram-negative, facultatively anaerobic, rod-shaped bacteria whose organisms arrange singly, in pairs, or short chains. This genus is commonly found in the intestinal tract and is an opportunistic pathogen that can give rise to bacteremia, pneumonia, urinary tract and several other types of human infection.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Anaerobic degradation of GLUCOSE or other organic nutrients to gain energy in the form of ATP. End products vary depending on organisms, substrates, and enzymatic pathways. Common fermentation products include ETHANOL and LACTIC ACID.
Tests of chemical substances and physical agents for mutagenic potential. They include microbial, insect, mammalian cell, and whole animal tests.
Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs.
The covalent bonding of an alkyl group to an organic compound. It can occur by a simple addition reaction or by substitution of another functional group.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria that occurs in soil, fecal matter, and sewage. It is an opportunistic pathogen and causes cystitis and pyelonephritis.
Gram-negative gas-producing rods found in feces of humans and other animals, sewage, soil, water, and dairy products.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
A computer simulation technique that is used to model the interaction between two molecules. Typically the docking simulation measures the interactions of a small molecule or ligand with a part of a larger molecule such as a protein.
A dioxygenase with specificity for the oxidation of the indoleamine ring of TRYPTOPHAN. It is an extrahepatic enzyme that plays a role in metabolism as the first and rate limiting enzyme in the kynurenine pathway of TRYPTOPHAN catabolism.
The usually underground portions of a plant that serve as support, store food, and through which water and mineral nutrients enter the plant. (From American Heritage Dictionary, 1982; Concise Dictionary of Biology, 1990)
A plant genus of the family ARACEAE. Members contain beta-glucosidases and trypsin inhibitors.
Eighteen-carbon cyclopentyl polyunsaturated fatty acids derived from ALPHA-LINOLENIC ACID via an oxidative pathway analogous to the EICOSANOIDS in animals. Biosynthesis is inhibited by SALICYLATES. A key member, jasmonic acid of PLANTS, plays a similar role to ARACHIDONIC ACID in animals.
A plant genus of the family LOGANIACEAE (classified by some botanists as Gelsemiaceae). The sometimes used common name of trumpet flower is also used for DATURA.
A serotype of Salmonella enterica that is a frequent agent of Salmonella gastroenteritis in humans. It also causes PARATYPHOID FEVER.

Induction of AT-specific DNA-interstrand crosslinks by bizelesin in genomic and simian virus 40 DNA. (1/9500)

Bizelesin is a bifunctional AT-specific DNA alkylating drug. Our study characterized the ability of bizelesin to induce interstrand crosslinks, a potential lethal lesion. In genomic DNA of BSC-1 cells, bizelesin formed from approx. 0.3 to 6.03+/-0.85 interstrand crosslinks per 106 base pairs, at 5-100 nM drug concentration, respectively, comparable to the number of total adducts previously determined in the same system (J.M. Woynarowski, M.M. McHugh, L.S. Gawron, T.A. Beerman, Biochemistry 34 (1995) 13042-13050). Bizelesin did not induce DNA-protein crosslinks or strand breaks. A model defined target, intracellular simian virus 40 (SV40) DNA, was employed to map at the nucleotide level sites of bizelesin adducts, including potential interstrand crosslinks. Preferential adduct formation was observed at AT tracts which are abundant in the SV40 matrix associated region and the origin of replication. Many sites, including each occurrence of 5'-T(A/T)4A-3', co-mapped on both DNA strands suggesting interstrand crosslinks, although monoadducts were also formed. Bizelesin adducts in naked SV40 DNA were found at similar sites. The localization of bizelesin-induced crosslinks in AT-rich tracts of replication-related regions is consistent with the potent anti-replicative properties of bizelesin. Given the apparent lack of other types of lesions in genomic DNA, interstrand crosslinks localized in AT-rich tracts, and to some extent perhaps also monoadducts, are likely to be lethal effects of bizelesin.  (+info)

Prior exposure to neurotrophins blocks inhibition of axonal regeneration by MAG and myelin via a cAMP-dependent mechanism. (2/9500)

MAG is a potent inhibitor of axonal regeneration. Here, inhibition by MAG, and myelin in general, is blocked if neurons are exposed to neurotrophins before encountering the inhibitor; priming cerebellar neurons with BDNF or GDNF, but not NGF, or priming DRG neurons with any of these neurotrophins blocks inhibition by MAG/myelin. Dibutyryl cAMP also overcomes inhibition by MAG/myelin, and cAMP is elevated by neurotrophins. A PKA inhibitor present during priming abrogates the block of inhibition. Finally, if neurons are exposed to MAG/myelin and neurotrophins simultaneously, but with the Gi protein inhibitor, inhibition is blocked. We suggest that priming neurons with particular neurotrophins elevates cAMP and activates PKA, which blocks subsequent inhibition of regeneration and that priming is required because MAG/myelin activates a Gi protein, which blocks increases in cAMP. This is important for encouraging axons to regrow in vivo.  (+info)

Single synaptic events evoke NMDA receptor-mediated release of calcium from internal stores in hippocampal dendritic spines. (3/9500)

We have used confocal microscopy to monitor synaptically evoked Ca2+ transients in the dendritic spines of hippocampal pyramidal cells. Individual spines respond to single afferent stimuli (<0.1 Hz) with Ca2+ transients or failures, reflecting the probability of transmitter release at the activated synapse. Both AMPA and NMDA glutamate receptor antagonists block the synaptically evoked Ca2+ transients; the block by AMPA antagonists is relieved by low Mg2+. The Ca2+ transients are mainly due to the release of calcium from internal stores, since they are abolished by antagonists of calcium-induced calcium release (CICR); CICR antagonists, however, do not depress spine Ca2+ transients generated by backpropagating action potentials. These results have implications for synaptic plasticity, since they show that synaptic stimulation can activate NMDA receptors, evoking substantial Ca2+ release from the internal stores in spines without inducing long-term potentiation (LTP) or depression (LTD).  (+info)

Role of dexamethasone dosage in combination with 5-HT3 antagonists for prophylaxis of acute chemotherapy-induced nausea and vomiting. (4/9500)

Dexamethasone (20 mg) or its equivalent in combination with 5-HT3 antagonists appears to be the gold-standard dose for antiemetic prophylaxis. Additional to concerns about the use of corticosteroids with respect to enhanced tumour growth or impaired killing of the tumour cells, there is evidence that high-dosage dexamethasone impairs the control of delayed nausea and emesis, whereas lower doses appear more beneficial. To come closer to the most adequate dose, we started a prospective, single-blind, randomized trial investigating additional dosage of 8 or 20 mg dexamethasone to tropisetron (Navoban), a 5-HT3 receptor antagonist, in cis-platinum-containing chemotherapy. After an interim analysis of 121 courses of chemotherapy in 69 patients, we have been unable to detect major differences between both treatment alternatives. High-dose dexamethasone (20 mg) had no advantage over medium-dose dexamethasone with respect to objective and subjective parameters of acute and delayed nausea and vomiting. In relation to concerns about the use of corticosteroids in non-haematological cancer chemotherapy, we suggest that 8 mg or its equivalent should be used in combination with 5-HT3 antagonists until further research proves otherwise.  (+info)

Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. (5/9500)

LY315920 is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, LY315920 inhibited sPLA2 activity with an IC50 of 9 +/- 1 nM or 7.3 x 10(-6) mole fraction, which approached the stiochiometric limit of this assay. The true potency of LY315920 was defined using a deoxycholate/phosphatidylcholine assay with a mole fraction of 1.5 x 10(-6). LY315920 was 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase. Human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by LY315920 with an IC50 of 0.79 microM. The release of TXA2 from these cells by N-formyl-methionyl-leucyl-phenylalanine or arachidonic acid was not inhibited. The i.v. administration of LY315920, 5 min before harvesting the bronchoalveolar lavage cells, resulted in the inhibition of sPLA2-induced production of TXA2 with an ED50 of 16.1 mg/kg. Challenge of guinea pig lung pleural strips with sPLA2 produced contractile responses that were suppressed in a concentration-dependent manner by LY315920 with an apparent KB of 83 +/- 14 nM. Contractile responses induced by arachidonic acid were not altered. Intravenous or oral administration of LY315920 to transgenic mice expressing the human sPLA2 protein inhibited serum sPLA2 activity in a dose-related manner over a 4-h time course. LY315920 is a potent and selective sPLA2 inhibitor and represents a new class of anti-inflammatory agent designated SPI. This agent is currently undergoing clinical evaluation and should help to define the role of sPLA2 in various inflammatory disease states.  (+info)

Glomerular size-selective dysfunction in NIDDM is not ameliorated by ACE inhibition or by calcium channel blockade. (6/9500)

BACKGROUND: In patients with insulin-dependent diabetes mellitus (IDDM) and overt nephropathy glomerular barrier size-selectivity progressively deteriorates with time and is effectively improved by angiotensin converting enzyme (ACE) inhibition. Whether similar glomerular functional changes develop in proteinuric patients with non-insulin-dependent diabetes mellitus (NIDDM), and whether antihypertensive agents can favorably affect glomerular filtration of macromolecules in these patients, has not been documented yet. METHODS: We investigated renal hemodynamics and fractional clearance of neutral dextrans of graded sizes, in nine proteinuric patients with NIDDM and renal biopsy findings of typical diabetic glomerulopathy. Six healthy volunteers served as controls. We also investigated the effects of an ACE inhibitor and of a calcium channel blocker, both given in doses targeted to achieve a comparable level of systemic blood pressure control, on glomerular hemodynamics and sieving function. Theoretical analysis of glomerular macromolecule transport was adopted to evaluate intrinsic glomerular membrane permeability properties. RESULTS: Fractional clearance of large macromolecules (42 to 66 A in radius) was significantly higher in diabetic patients than in controls, and the distribution of membrane pore radii was calculated to be shifted towards larger pore sizes in diabetics (mean radius increased from 55 to 60 A). Despite effective blood pressure control, neither antihypertensive affected glomerular hemodynamics to any significant extent. Fractional clearance of dextrans, as well as of albumin and IgG, and total urinary proteins were not modified by either treatments. CONCLUSIONS: These data indicate that patients with NIDDM and overt nephropathy develop abnormalities in size-selective function of the glomerular barrier and, at variance to IDDM, such changes were not ameliorated either by ACE inhibition or calcium channel blockade.  (+info)

Involvement of p21 in the PKC-induced regulation of the G2/M cell cycle transition. (7/9500)

Activation of protein kinase C (PKC) inhibits cell cycle progression at the G1/S and G2/M transitions. We found that phorbol 12-myristate 13-acetate (PMA) induced upregulation of p21, not only in MCF-7 cells arrested in the G1 phase as previously shown, but also in cells delayed in the G2 phase. This increase in p21 in cells accumulated in the G1 and G2/M phases of the cell cycle after PMA treatment was inhibited by the PKC inhibitor GF109203X. This indicates that PKC activity is required for PMA-induced p21 upregulation and cell cycle arrest in the G1 and G2/M phases of the cell cycle. To further assess the role of p21 in the PKC-induced G2/M cell cycle arrest independently of its G1 arrest, we used aphidicolin-synchronised MCF-7 cells. Our results show that, in parallel with the inhibition of cdc2 activity, PMA addition enhanced the associations between p21 and either cyclin B or cdc2. Furthermore, we found that after PMA treatment p21 was able to associate with the active Tyr-15 dephosphorylated form of cdc2, but this complex was devoid of kinase activity indicating that p21 may play a role in inhibition of cdc2 induced by PMA. Taken together, these observations provide evidence that p21 is involved in integrating the PKC signaling pathway to the cell cycle machinery at the G2/M cell cycle checkpoint.  (+info)

Phosphatidylinositol 3-kinase and protein kinase C are required for the inhibition of caspase activity by epidermal growth factor. (8/9500)

The mechanism by which growth factors exert an anti-apoptotic function on many cell types is not well understood. This issue is addressed in relation to epidermal growth factor (EGF) which inhibits apoptosis induced by staurosporine or wortmannin in an epithelial tumour cell line (CNE-2). The presence of EGF substantially reduced the in vitro Ac-DEVD-AMC hydrolytic activity and almost completely suppressed the intracellular cleavage of poly(ADP-ribose) polymerase in staurosporine- or wortmannin-treated cells. Staurosporine but not wortmannin caused the intracellular proteolytic processing of pro-caspase-3 and this event was transiently inhibited by EGF. Staurosporine-induced apoptosis was not inhibited by EGF in the presence of wortmannin or LY294002. Similarly, EGF failed to inhibit wortmannin-induced apoptosis in the presence of staurosporine, chelerythrine chloride or Go6850. These results suggest that phosphatidylinositol 3-kinase and protein kinase C play a role in the survival function of EGF but the reduction of cellular caspase activity cannot be satisfactorily explained by a lack of pro-caspase-3 activation.  (+info)

Bartoli indole synthesis Bischler-Möhlau indole synthesis Cadogan-Sundberg indole synthesis Fukuyama indole synthesis Gassman ... Indoles are susceptible to hydrogenation of the imine subunit. Indole-3-butyric acid Indole test Isoindole Isoindoline Martinet ... The Leimgruber-Batcho indole synthesis is an efficient method of synthesizing indole and substituted indoles. Originally ... Although the synthesis of indole itself is problematic using the Fischer indole synthesis, it is often used to generate indoles ...
Some 200 dimeric indole alkaloids are known with two indole groups. The number of known non-isoprenoid indole alkaloids is ... Indole alkaloids are a class of alkaloids containing a structural moiety of indole; many indole alkaloids also include isoprene ... Simple derivatives of indole Simple derivatives of β-carboline Pyrroloindole alkaloids Indole-3-carbinol Indole-3-acetic acid ... Indole alkaloids are distinguished depending on their biosynthesis. The two types of indole alkaloids are isoprenoids and non- ...
This is due to the presence of skatole, also known as methyl indole or methylated indole, another possible product of ... The Indole test is one of the four tests of the IMViC series, which tests for evidence of an enteric bacterium. The other three ... The indole test is a biochemical test performed on bacterial species to determine the ability of the organism to convert ... Example of typical indole reactions Angen, O.; Mutters, R.; Caugant, D. A.; Olsen, J. E.; Bisgaard, M. (1999). "Taxonomic ...
Bartoli indole synthesis Japp-Klingemann indole synthesis Leimgruber-Batcho indole synthesis Larock indole synthesis Madelung ... The Fischer indole synthesis is a chemical reaction that produces the aromatic heterocycle indole from a (substituted) ... Wagaw, S.; Yang, B. H.; Buchwald, S. L. (1998). "A Palladium-Catalyzed Strategy for the Preparation of Indoles: A Novel Entry ... Via a palladium-catalyzed reaction, the Fischer indole synthesis can be effected by cross-coupling aryl bromides and hydrazones ...
The Hemetsberger indole synthesis (also called the Hemetsberger-Knittel synthesis) is a chemical reaction that thermally ... Gribble, G. W. (2000). "Recent developments in indole ring synthesis-methodology and applications". J. Chem. Soc., Perkin Trans ... decomposes a 3-aryl-2-azido-propenoic ester into an indole-2-carboxylic ester. Yields are typically above 70%. However, this is ...
The Hegedus indole synthesis is a name reaction in organic chemistry that allows for the generation of indoles through ... 2-Allylaniline can be converted to 2-Methylindole using the Hegedus indole synthesis. Hegedus, Louis S.; Allen, Gary F.; ... ISBN 978-3-540-30030-4. v t e (Ring forming reactions, Indole forming reactions, Carbon-heteroatom bond forming reactions, Name ... A new synthesis of indoles". Journal of the American Chemical Society. 98 (9): 2674-2676. doi:10.1021/ja00425a051. Hegedus, ...
... indole-3-carbinol) found in human diet was claimed by Dashwood et al. in 1989. Indole-3-carbinol induces a G1 growth arrest of ... a fact that can be used to design clinical trial to treat human patients with indole-3-carbinol in future. Indole-3-carbinol ... to determine if supplemental indole-3-carbinol has health benefits. Investigation of mechanisms by which consumption of indole- ... Overuse of indole-3-carbinol supplements in the hope of preventing cancer may be unwise, as the hormone balance should be ...
The Gassman indole synthesis is a series of chemical reactions used to synthesize substituted indoles by addition of an aniline ... Gassman, P. G.; van Bergen, T. J.; Gilbert, D. P.; Cue, Jr., B. W. (1974). "General method for the synthesis of indoles". J. Am ... Synthesis of indoles, oxindoles, and alkylated aromatic amines bearing cation stabilizing substituents". J. Am. Chem. Soc. 96 ( ... The 3-position thiomethyl group is often removed using Raney nickel to give the 3-H-indole. The reaction mechanism of the ...
3-disubstituted indoles. A practical one-pot reaction that can be useful for the creation of disubstituted indoles. Most ... the application of the Fukuyama Indole synthesis to create a disubstituted indole. In addition, the fukuyama reaction plays a ... The Fukuyama Indole synthesis can generate a range of different substituents at the 2,3 position that were previously ... The Fukuyama indole synthesis is a versatile tin mediated chemical reaction that results in the formation of 2, ...
The Leimgruber-Batcho indole synthesis gives similar flexibility and regiospecificity to indole derivatives. One advantage of ... which is difficult to do with the Leimgruber-Batcho indole synthesis. The reaction mechanism of the Bartoli indole synthesis is ... to give a dimagnesium indole salt (12). Reaction workup eliminates water and gives the final desired indole (13). Therefore, ... The Bartoli indole synthesis (also called the Bartoli reaction) is the chemical reaction of ortho-substituted nitroarenes and ...
... belongs to the class of organic compounds known as indoles. These are compounds containing an indole ... Indole-3-acetaldehyde is a substrate for retina-specific copper amine oxidase, aldehyde dehydrogenase X (mitochondrial), amine ... Nutaratat P, Srisuk N, Arunrattiyakorn P, Limtong S (2016). "Indole-3-acetic acid biosynthetic pathways in the basidiomycetous ...
The Reissert indole synthesis is a series of chemical reactions designed to synthesize indole or substituted-indoles (4 and 5) ... Leimgruber-Batcho indole synthesis Reissert, A. (1897). "Einwirkung von Oxalester und Natriumäthylat auf Nitrotoluole. Synthese ... V. The Structure of Certain Indole Derivatives Related to Gliotoxin1,2". J. Am. Chem. Soc. 67 (3): 423. doi:10.1021/ja01219a023 ... Butin, Alexander; Stroganova, Tatyana; Lodina, Irina; Krapivin, Gennady (2001). "Furan ring opening-indole ring closure: a new ...
The Larock indole synthesis is a heteroannulation reaction that uses palladium as a catalyst to synthesize indoles from an ... Indoles are one of the most prevalent heterocyclic structures found in biological processes, so the production of indole ... also derived 2- and 2,3-substituted indoles without using LiCl. The optimized Indole reaction uses 10% Pd/C (3.0 mol%) with 1.1 ... The reaction is extremely versatile and can be used to produce varying types of indoles. Larock indole synthesis was first ...
Other solid-phase indole syntheses were also reported, some of which use different scaffolds and metal catalysts to drive the ... There are also a variety of other reactions that result in the same indole skeleton. In a review article, Taber et al. ... The Nenitzescu indole synthesis is a chemical reaction that forms 5-hydroxyindole derivatives from benzoquinone and β- ... Huang, Yun-Sheng; Zhang, W.; Zhang, X.; Wang, J. (2010). "Manufacturing synthesis of 5-hydroxy-2-methyl-1H-indole". Research on ...
... (EC, BX2 (gene), CYP71C4 (gene)) is an enzyme with systematic name indole,NAD(P)H:oxygen ... Indole-2-monooxygenase at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: Biology (Articles with ... H2O Indole-2-monooxygenase is involved in the biosynthesis of protective and allelopathic benzoxazinoids in some plants. Frey M ... oxidoreductase (2-hydroxylating). This enzyme catalyses the following chemical reaction indole + NAD(P)H + H+ + O2 ⇌ {\ ...
... (I3A), also known as indole-3-aldehyde and 3-formylindole, is a metabolite of dietary L-tryptophan which ... Indole-3-carbaldehyde has reactivity typical of aromatic aldehydes. It can is easily oxidized to indole-3-carboxylic acid. It ... Molecular mechanisms of action of indole and its metabolites on host physiology and disease "Indole-3-carboxaldehyde". PubChem ... Indole-3-propionic acid (IPA)] has previously been identified in the plasma and cerebrospinal fluid of humans, but its ...
Buu-Hoï Modified Indole Synthesis Blackhall and Thomson Modified Indole Synthesis Japp and Murray Modified Indole Synthesis The ... Fischer indole synthesis Bischler-Napieralski reaction "Bischler Indole Synthesis", Indole Ring Synthesis: From Natural ... The Bischler-Möhlau indole synthesis, also often referred to as "The Bischler Indole Synthesis," is a chemical reaction that ... the general indole synthesis process was given the name "Bischler-Möhlau Indole Synthesis." This original procedure for the ...
Bartoli indole synthesis Fischer indole synthesis Reissert indole synthesis ^ Batcho, A. D.; Leimgruber, W. U.S. Patent ... The Leimgruber-Batcho indole synthesis is a series of organic reactions that produce indoles from o-nitrotoluenes 1.[1][2][3] ... Many indoles are pharmacologically active, so a good indole synthesis is important for the pharmaceutical industry. The process ... Indole forming reactions, Carbon-heteroatom bond forming reactions, Name reactions). ...
... (6-API, 6-IT) is an indole derivative which was first identified being sold on the designer drug market ... "The effects of an indole derivative 692'-amino-propyl indole) on the general and coronary haemodynamics of the intact dog". ... This is the 5-isomer, 5-(2-aminopropyl)indole or 5-IT"[1]. Studies in dogs have also shown the drug to increase hemoglobin ... as indole rings are not included as rings under the 2-phenethylamine derived section of the NPsG. "New Psychoactive Substances ...
... is an indolequinone, a chemical compound found in the oxidative browning reaction of fruits like bananas ...
... indol-3-yl)pyruvate + NADPH + H+ + O2 ⇌ {\displaystyle \rightleftharpoons } (indol-3-yl)acetate + NADP+ + H2O + CO2 Indole-3- ... Indole-3-pyruvate monooxygenase (EC, YUC2 (gene), spi1 (gene)) is an enzyme with systematic name indole-3-pyruvate, ... Indole-3-pyruvate+monooxygenase at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: Biology v t e ( ... Zhao Y (March 2012). "Auxin biosynthesis: a simple two-step pathway converts tryptophan to indole-3-acetic acid in plants". ...
Sulphide Indole Motility (SIM) medium is a bacterial growth medium which tests for the ability to reduce sulfates, the ability ... to produce indoles, and motility. This combination of challenges in one mixture is convenient and commercially available in ...
In enzymology, an indole-3-acetaldehyde oxidase (EC is an enzyme that catalyzes the chemical reaction (indol-3-yl) ... indol-3-yl)acetaldehyde, H2O, and O2, whereas its two products are (indol-3-yl)acetate and H2O2. This enzyme belongs to the ... Koshiba T, Matsuyama H (1993). "An in Vitro System of Indole-3-Acetic Acid Formation from Tryptophan in Maize (Zea mays) ... The systematic name of this enzyme class is (indol-3-yl)acetaldehyde:oxygen oxidoreductase. Other names in common use include ...
The Baeyer-Emmerling indole synthesis is a method for synthesizing indole from a (substituted) ortho-nitrocinnamic acid and ... Decarboxylation gives indole. Baeyer-Drewson indigo synthesis Bayer, A.; Emmerling, A. (1869). "Synthese des indoles" [ ... Ring forming reactions, Indole forming reactions, Organic reactions, Name reactions). ... Synthesis of indoles]. Berichte der deutschen chemischen Gesellschaft. 2 (1): 679-682. doi:10.1002/cber.186900201268. Baeyer 5 ...
... (EC is an enzyme with systematic name indole-3-carboxylate carboxy-lyase. This ... Indole-3-carboxylate+decarboxylase at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: Biology (EC ... Yoshida T, Fujita K, Nagasawa T (November 2002). "Novel reversible indole-3-carboxylate decarboxylase catalyzing nonoxidative ... enzyme catalyses the following chemical reaction indole-3-carboxylate ⇌ {\displaystyle \rightleftharpoons } indole + CO2 This ...
Indole dioxygenase is not specific to indole but rather operates on a broad range of indole derivatives, including the amino ... Other names in common use include indole oxidase, indoleamine 2,3-dioxygenase (ambiguous), indole:O2 oxidoreductase, indole- ... In enzymology, an indole 2,3-dioxygenase (EC is an enzyme that catalyzes the chemical reaction indole + O2 ⇌ {\ ... Nair PM; Vaidyanathan CS (1964). "An indole oxidase isolated from the leaves of Tecoma stans". Biochim. Biophys. Acta. 81 (3): ...
... indole ⇌ {\displaystyle \rightleftharpoons } L-tryptophan + H2O This enzyme salvages the lost indole to L-tryptophan. Hettwer S ... Tryptophan synthase (indole-salvaging) (EC, tryptophan synthase beta2) is an enzyme with systematic name L-serine ... Tryptophan+synthase+(indole-salvaging) at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: Biology ( ... hydro-lyase (adding indole, L-tryptophan-forming). This enzyme catalyses the following chemical reaction L-serine + ...
"1H-Indole-3-acetic acid" Registry of Toxic Effects of Chemical Substances (RTECS). Page last updated:November 8, 2017. "Indole- ... Plants mainly produce IAA from tryptophan through indole-3-pyruvic acid. IAA is also produced from tryptophan through indole-3- ... Indole-3-acetic acid (IAA, 3-IAA) is the most common naturally occurring plant hormone of the auxin class. It is the best known ... Jeong YM, Oh MH, Kim SY, Li H, Yun HY, Baek KJ, Kwon NS, Kim WY, Kim DS (2010). "Indole-3-acetic acid/horseradish peroxidase ...
... (1H-indole-3-butanoic acid, IBA) is a white to light-yellow crystalline solid, with the molecular formula ... Ludwig-Müller, J. (2000). "Indole-3-butyric acid in plant growth and development". Plant Growth Regulation. Vol. 32, no. 2-3. ... 1.{{cite news}}: CS1 maint: multiple names: authors list (link) Ludwig-Müller, J. (2000). "Indole-3-butyric acid in plant ... "Identification and characterization of Arabidopsis indole-3-butyric acid response mutants defective in novel peroxisomal ...
The Cadogan-Sundberg indole synthesis, or simply Cadogan indole synthesis, is a name reaction in organic chemistry that allows ... Gribble, Gordon W. (17 June 2016). "Cadogan-Sundberg Indole Synthesis". Indole Ring Synthesis: From Natural Products to Drug ... Li, Jie Jack (4 January 2014). "Cadogan-Sundberg indole synthesis". Indole Ring Synthesis: From Natural Products to Drug ... which reacts again with triethyl phosphite to form the indole. The Cadogan-Sundberg indole synthesis has been used as an ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
Indole-5-carboxaldehyde 0.98; CAS No.: 1196-69-6; Synonyms: 5-Formylindole; Linear Formula: C9H7NO; Empirical Formula: C9H7NO; ... Indole-5-carboxaldehyde can be used as a reactant in the:. *Preparation of curcumin derivatives as anti-proliferative & anti- ... Synthesis of (5-(4-(3,4,5-trimethoxybenzoyl)-1H-imidazol-2-yl)-1H-indol-2-yl)(3,4,5-trimethoxyphenyl)methanone. and ...
Testing Status of Indole-3-carbinol M990063. Testing Status of Indole-3-carbinol M990063. CASRN: 700-06-1. Formula: C9-H9-N-O. ... Toxicology Studies of Indole-3-Carbinol (CASRN 700-06-1) in F344/N Rats and B6C3F1/N Mice and Toxicology and Carcinogenesis ... Studies of Indole-3-Carbinol in Harlan Sprague Dawley Rats and B6C3F1/N Mice (Gavage Studies) ...
Structure, properties, spectra, suppliers and links for: 2-Cyclohexyl-1H-indole, 13141-48-5.
The structure of isolated compounds from P. methysticum G. Forst and V. officinalis L. contains an indole moiety. The indole ... The structure of isolated compounds from P. methysticum G. Forst and V. officinalis L. contains an indole moiety. The indole ... Hence, the objective of this review is to discuss bioactive compounds containing the indole moiety from plants that can serve ... Hence, the objective of this review is to discuss bioactive compounds containing the indole moeity from plants that can serve ...
... Molecular Formula: C12H16N2 ...
indole derivative biosynthesis; indole derivative biosynthetic process; indole-containing compound anabolism; indole-containing ... The chemical reactions and pathways resulting in the formation of compounds that contain an indole (2,3-benzopyrrole) skeleton. ...
... indole , C21H23NO2 , CID 56841530 - structure, chemical names, physical and chemical properties, classification, patents, ...
6PYU: Human PI3Kdelta in complex with Compound 4-2 ((3S)-1-(cyclopropanecarbonyl)-5-(quinoxalin-6-yl)spiro[indole-3,2- ... 3S)-1-(cyclopropanecarbonyl)-5-(quinoxalin-6-yl)spiro[indole-3,2-pyrrolidin]-2(1H)-one. ...
... indole (IND), 3-methyl indole (3-MI), 2-methyl indole (2-MI), or 1-methyl indole (1-MI) at a concentration of 20 μM. (C) The ... The predicted two indole-binding model in (C) hAHR and (D) mAHR ligand binding domain. The predicted two 3-methyl indole- ... or indole/ methyl indole isomers (100 μM) with or without the addition of IL1B (10 ng/mL). (E) In vitro translated AHR/ARNT gel ... or indole/methyl indole isomers (100 μM) and 3 h incubation with luciferin-CEE reagent. (D) Synergistic IL6 expression within ...
Desde cria me costo coger la energia en las relaciones de todo indole. Home » Desde cria me costo coger la energia en las ... Desde cria me costo coger la energia en las relaciones de todo indole2022-07-292022-07-29/wp-content/uploads/2019/10/re-logo-1- ... Desde cria me costo coger la energia en las relaciones de todo indole. By Admin ...
Additionally, the indole moiety of one of the novel inhibitors binds in a region, close to the peripheral anionic site of the ... Galantamine derivatives with indole moiety: Docking, design, synthesis and acetylcholinesterase inhibitory activity Mariyana ... Galantamine derivatives with indole moiety: Docking, design, synthesis and acetylcholinesterase inhibitory activity Mariyana ... The novel galantamine derivatives with indole moiety have dual site binding to the enzyme--the galantamine moiety binds to the ...
Ketone, indol-1-yl ethyl. Change simulation parameters The result was obtained by a proprietary SIELC algorithm. It may deviate ... Ketone, indol-1-yl ethyl can be analyzed by this reverse phase (RP) HPLC method with simple conditions. The mobile phase ... Separation of Ketone, indol-1-yl ethyl on Newcrom R1 HPLC column. May 16, 2018. ...
We then tested indole-3-tetrazole against the AFB5 homologue of TIR1, finding that binding was selective against TIR1, absent ... 9 more authors) (2018) The tetrazole analogue of the auxin indole-3-acetic acid binds preferentially to TIR1 and not AFB5. ACS ... The basis of the preference of indole-3-tetrazole for TIR1 was revealed to be a single residue substitution using molecular ... The tetrazole analogue of the auxin indole-3-acetic acid binds preferentially to TIR1 and not AFB5 ...
1-(tert-Butoxycarbonyl)-1H-indol-3-yl)boronic acid, , 181365-26-4, NO MDL FOUND ...
Metabolite indole_p in iECO26_1355. Indole.
5E)-1-benzoyl-2,2a,3,4-tetrahydrobenzo[cd]indol-5(1H)-one oxime - C18H16N2O2, synthesis, structure, density, melting point, ... indol-5(1H)-one oxime , density of (5E)-1-benzoyl-2,2a,3,4-tetrahydrobenzo[cd]indol-5(1H)-one oxime , refractive index of (5E)- ... Tags: melting point of (5E)-1-benzoyl-2,2a,3,4-tetrahydrobenzo[cd]indol-5(1H)-one oxime , boiling point of (5E)-1-benzoyl-2,2a, ... 5E)-1-benzoyl-2,2a,3,4-tetrahydrobenzo[cd]indol-5(1H)-one oxime. ... 4-amino-1-benzoyl-2,2a,3,4-tetrahydrobenzo[cd]indol-5(1H)-one ...
7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid. An open source of chemical information ... trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid. ...
HOLOVR releases Nothing is Whole on Indole Records. By Tom Durston BUY Reading Time: 1 min ... ArtistHOLOVRLabelIndole RecordsReleased5 March 2021GenreAmbientDroneElectronicExperimental ... Nothing is Whole is out now via Indole Records. Order a copy from Bandcamp. ... the London-based producer marks his return as HOLOVR with a new nine-track album on Indole Records. ...
Molecular modeling based on a subsequently obtained cryo-EM structure of p97 in complex with a phenyl indole was used to ... Optimization of the side-chain of a phenyl indole scaffold identified from a high-throughput screening campaign for inhibitors ... Molecular modeling based on a subsequently obtained cryo-EM structure of p97 in complex with a phenyl indole was used to ... Optimization of the side-chain of a phenyl indole scaffold identified from a high-throughput screening campaign for inhibitors ...
Click the button below to add the 1-Ethyl-2,3-dihydro-1H-indole-5-carbaldehyde 1g to your wish list. ...
... and methods of treating various medical disorders using such indoles and pharmaceutical compositions thereof. ... The present invention provides sulfonamide-substituted indoles and Methods of Use Thereof-substituted pyrrolopyridines, ... Step 1: 3-Bromo-1-methyl-5-nitro-1H-indole. To a solution 3-bromo-5-nitro-1H-indole (5.5 g, 20.6 mmol) in THF (50 mL) at 0° C. ... R)-N-(1-methyl-3-(1-(2,3,3- trimethylbutanoyl)piperidin-4-yl)-1H-indol-5- yl)benzenesulfonamide. LCMS: m/e 482.2 [M + H]+ 30 (R ...
1. On the Electron-Donating Properties of Indoles Publication: National Academy of Sciences (U.S.), 15 October 1960 Subject(s ...
Open Beauty Facts est développé par une association à but non lucratif indépendante de lindustrie. Open Food Facts est fait pour tous, par tous, et est financé par tous. Vous pouvez soutenir notre travail en donnant à Open Beauty Facts et aussi en utilisant le moteur de recherche Lilo ...
In this study, Szent-Gyorgyi and Isenberg examined the charge-transfer behavior of indole, and speculated about why indole and ... On the Electron-Donating Properties of Indoles. Contributor(s):. Proceedings of the National Academy of Sciences of the United ... even though indoles structure does not predict such reactivity. Copyright:. This item may be under copyright protection; ... some indole derivatives (such as serotonin and tryptophan) readily form charge-transfer complexes with substances like ...
Indoles and derivatives. Sub Class. Indoles. Direct Parent. 3-alkylindoles. Alternative Parents. Monoalkyl phosphates / ... 1-C-(indol-3-yl)glycerol 3-phosphate (CHEBI:51793) Affected organisms. Not Available. Chemical Identifiers. UNII. Not Available ... Indole-3-Glycerol Phosphate. DrugBank Accession Number. DB04143. Background. Not Available. Type. Small Molecule. Groups. ... The beta subunit is responsible for the synthesis of L-tryptophan from indole and L-serine.. Gene Name. trpB. Uniprot ID. ...
Indoles. May prevent carcinogens from reaching their intended goal inside of cells. See also sulforaphane. ...
Indoles. May prevent carcinogens from reaching their intended goal inside of cells. See also sulforaphane. ...
... references and reaction samples of the Cadogan-Sundberg Indole Synthesis ...
  • Indole derivatives targeting colchicine binding site as potential anticancer agents. (
  • Several studies have reported design, synthesis, and biological evaluation of indole derivatives as potential anticancer agents . (
  • The present work has reviewed indole derivatives as potential colchicine - binding site inhibitors. (
  • The structure-activity relationship studies have revealed the crucial pharmacophoric features required for the potent and selective binding of indole derivatives to the CBS. (
  • Results: The screening study from a small library consisting of benzimidazole and indole derivatives discovered a compound (CZ74) with an indole-core structure. (
  • Click the button below to add the Methyl 3h-benzo[e]indole-2-carboxylate 250 mg to your wish list. (
  • Indole-3-carbinol, the powerful phytochemical found in cruciferous vegetables, provides support for healthy breast, cervical and prostate cells. (
  • In the other tube, the tests for indole production, ornithine decarboxylase, and motility are conducted. (
  • These are compounds containing an indole moiety that carries an alkyl chain at the 3-position. (
  • Indole-3-Carbinol dietary supplement provides compounds found in vegetables to help support healthy breast, cervical and prostate cells. (
  • The (βα) 8 -barrel enzyme indole-3-glycerol phosphate synthase (IGPS) catalyzes the multistep transformation of 1-(o- carboxyphenylamino)-1-deoxyribulose 5-phosphate (CdRP) into indole-3-glycerol phosphate (IGP) in tryptophan biosynthesis. (
  • Conclusion: This indole-cored molecule CZ74 could be a potential lead compound and could be further developed as a new generation of antibacterial agents targeting FtsZ to combat against multidrug-resistant bacteria. (
  • Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97. (
  • Optimization of the side-chain of a phenyl indole scaffold identified from a high-throughput screening campaign for inhibitors of the AAA+ ATPase p97 is reported. (
  • Molecular modeling based on a subsequently obtained cryo-EM structure of p97 in complex with a phenyl indole was used to rationalize the potency of these allosteric inhibitors. (
  • Indole oxidation represents a real challenge for selectivity because it typically leads to complex mixtures of products even when highly selective enzymes are used. (
  • Mn-MC6*a promotes the selective oxidation of indole at its C3 position, leading to a 3-oxindole derivative (2-TFE-3-oxindole) with unprecedented product selectivity (86% at pH 8.5) compared to native or artificial heme-enzymes. (
  • We also suggest a possible reaction mechanism based on the effect of pH, cosolvent, and indole substitution on the reaction outcome. (
  • These antioxidant properties can be utilized toreduce the occurrence of chronic diseases and provide many health benefits in humans.Phytochemicals such as Indoles, plant sterols, flavonoids and lignans have beenextracted and studied widely. (
  • Here, we describe the catalytic potential of an artificial enzyme, Mn-Mimochrome VI*a (Mn-MC6*a), in promoting indole oxidation. (
  • Indole-3-carbinol (I3C), naturally found in vegetables including broccoli, brussels sprouts and cabbage, supports the function of healthy breast cells. (
  • In this study, Szent-Gyorgyi and Isenberg examined the charge-transfer behavior of indole, and speculated about why indole and some indole derivatives (such as serotonin and tryptophan) readily form charge-transfer complexes with substances like riboflavin, even though indole's structure does not predict such reactivity. (
  • Novel and promising anti-Gram-negative antimicrobials belong both to old (cephalosporins, carbapenems, β-lactamase inhibitors, monobactams, aminoglycosides, polymyxin analogues and tetracycline) and completely new antibacterial classes (boron-containing antibacterial protein synthesis inhibitors, bis-indoles, outer membrane synthesis inhibitors, antibiotics targeting novel sites of the 50S ribosomal subunit and antimicrobial peptides). (
  • Herein, a series of 20 1 H -indoles were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. (
  • An overview of Genetic Toxicology Micronucleus Rats study conclusions related to Indole-3-carbinol (700-06-1). (
  • Here, we find that, unlike the phytocannabinoid Δ 9 -tetrahydrocannabinol, the indole-moiety containing SCs, AM2201 and JWH-018, act as positive allosteric modulators (PAMs) at the 5-HT 1A receptor (5-HT 1A R). This suggests that some biological effects of SCs might involve allosteric interactions with 5-HT 1A Rs. (
  • In this study, four new prenylated indole- terpenoids (1-4), named encindolenes I-L, as well as a known analogue (5), were isolated from the fungus Penicillium sp. (
  • New classes of environmental tumor promoters: indole alkaloids and polyacetates. (