Acetamides: Derivatives of acetamide that are used as solvents, as mild irritants, and in organic synthesis.Etanidazole: A nitroimidazole that sensitizes hypoxic tumor cells that are normally resistant to radiation therapy.NitrofuransIodoacetamide: An alkylating sulfhydryl reagent. Its actions are similar to those of iodoacetate.Acetanilides: Compounds based on N-phenylacetamide, that are similar in structure to 2-PHENYLACETAMIDES. They are precursors of many other compounds. They were formerly used as ANALGESICS and ANTIPYRETICS, but often caused lethal METHEMOGLOBINEMIA.Formamides: A group of amides with the general formula of R-CONH2.Cryoprotective Agents: Substances that provide protection against the harmful effects of freezing temperatures.Phenoxypropanolamines: Compounds based on a propanolamine attached via an OXYGEN atom to a phenoxy ring. The side chain is one carbon longer than PHENYLETHYLAMINES.Hares: The genus Lepus, in the family Leporidae, order LAGOMORPHA. Hares are born above ground, fully furred, and with their eyes and ears open. In contrast with RABBITS, hares have 24 chromosome pairs.Amides: 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)Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Hydrocarbons, FluorinatedAmidohydrolasesThiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.Indoleacetic Acids: Acetic acid derivatives of the heterocyclic compound indole. (Merck Index, 11th ed)Urea: A compound formed in the liver from ammonia produced by the deamination of amino acids. It is the principal end product of protein catabolism and constitutes about one half of the total urinary solids.Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.Semen Preservation: The process by which semen is kept viable outside of the organism from which it was derived (i.e., kept from decay by means of a chemical agent, cooling, or a fluid substitute that mimics the natural state within the organism).Molecular Structure: 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.Iodoacetates: Iodinated derivatives of acetic acid. Iodoacetates are commonly used as alkylating sulfhydryl reagents and enzyme inhibitors in biochemical research.Alkylation: 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.Structure-Activity Relationship: 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.Glycerol: A trihydroxy sugar alcohol that is an intermediate in carbohydrate and lipid metabolism. It is used as a solvent, emollient, pharmaceutical agent, and sweetening agent.Cryopreservation: Preservation of cells, tissues, organs, or embryos by freezing. In histological preparations, cryopreservation or cryofixation is used to maintain the existing form, structure, and chemical composition of all the constituent elements of the specimens.Fluorine Radioisotopes: Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes.Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Pseudomonas: A genus of gram-negative, aerobic, rod-shaped bacteria widely distributed in nature. Some species are pathogenic for humans, animals, and plants.Pyrimidines: A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.Cell Membrane Permeability: A quality of cell membranes which permits the passage of solvents and solutes into and out of cells.Magnetic Resonance Spectroscopy: 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).Gas Chromatography-Mass Spectrometry: A microanalytical technique combining mass spectrometry and gas chromatography for the qualitative as well as quantitative determinations of compounds.ThiazolesReceptors, GABA-A: Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.Stereoisomerism: 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)Carbon Radioisotopes: Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Kinetics: The rate dynamics in chemical or physical systems.Water: A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Positron-Emission Tomography: An imaging technique using compounds labelled with short-lived positron-emitting radionuclides (such as carbon-11, nitrogen-13, oxygen-15 and fluorine-18) to measure cell metabolism. It has been useful in study of soft tissues such as CANCER; CARDIOVASCULAR SYSTEM; and brain. SINGLE-PHOTON EMISSION-COMPUTED TOMOGRAPHY is closely related to positron emission tomography, but uses isotopes with longer half-lives and resolution is lower.Culture Media: 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.Indoles: 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.Palladium: 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.Catalysis: The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.Alkenes: Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)Cyclization: Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Centrifugation, Density Gradient: Separation of particles according to density by employing a gradient of varying densities. At equilibrium each particle settles in the gradient at a point equal to its density. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Delayed-Action Preparations: Dosage forms of a drug that act over a period of time by controlled-release processes or technology.Polymers: Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).Chemistry, Pharmaceutical: Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.Technology, Pharmaceutical: The application of scientific knowledge or technology to pharmacy and the pharmaceutical industry. It includes methods, techniques, and instrumentation in the manufacture, preparation, compounding, dispensing, packaging, and storing of drugs and other preparations used in diagnostic and determinative procedures, and in the treatment of patients.Drug Compounding: The preparation, mixing, and assembling of a drug. (From Remington, The Science and Practice of Pharmacy, 19th ed, p1814)

delta-Aminolevulinate synthetases in the liver cytosol fraction and mitochondria of mice treated with allylisopropylacetamide and 3,5-dicarbethoxyl-1,4-dihydrocollidine. (1/1656)

Hepatic delta-aminolevulinate (ALA) synthetase was induced in mice by the administration of allylisopropylacetamide (AIA) and 3,5-dicarbethoxy-1,4-dihydrocollidine (DDC). In both cases, a significant amount of ALA synthetase accumulated in the liver cytosol fraction as well as in the mitochondria. The apparent molecular weight of the cytosol ALA synthetase was estimated to be 320,000 by gel filtration, but when the cytosol ALA synthetase was subjected to sucrose density gradient centrifugation, it showed a molecular weight of 110,000. In the mitochondria, there were two different sizes of ALA synthetase with molecular weights of 150,000 and 110,000, respectively; the larger enzyme was predominant in DDC-treated mice, whereas in AIA-treated mice and normal mice the enzyme existed mostly in the smaller form. When hemin was injected into mice pretreated with DDC, the molecular size of the mitochondrial ALA synthetase changed from 150,000 to 110,000. The half-life of ALA synthetase in the liver cytosol fraction was about 30 min in both the AIA-treated and DDC-treated mice. The half-life of the mitochondrial ALA synthetase in AIA-treated mice and normal mice was about 60 min, but in DDC-treated mice the half-life was as long as 150 min. The data suggest that the cytosol ALA synthetase of mouse liver is a protein complex with properties very similar to those of the cytosol ALA synthetase of rat liver, which has been shown to be composed of the enzyme active protein and two catalytically inactive binding proteins, and that ALA synthetase may be transferred from the liver cytosol fraction to the mitochondria with a size of about 150,000 daltons, followed by its conversion to enzyme with a molecular weight of 110,000 within the mitochondria. The process of intramitochondrial enzyme degradation seems to be affected in DDC-treated animals.  (+info)

Properties of 5-aminolaevulinate synthetase and its relationship to microsomal mixed-function oxidation in the southern armyworm (Spodoptera eridania). (2/1656)

1. Activity of 5-aminolaevulinate synthetase was measured in the midgut and other tissues of the last larval instar of the southern armyworm (Spodoptera eridania Cramer, formerly Prodenia eridania Cramer). 2. Optimum conditions for measuring the activity were established with respect to all variables involved and considerable differences from those reported for mammalian enzyme preparations were found. 3. Maximum activity (20 nmol/h per mg of protein) occurs 18-24 h after the fifth moult and thereafter decreases to trace amounts as the larvae age and approach pupation. 4. Synthetase activity was rapidly induced by oral administration (in the diet) of pentamethylbenzene, phenobarbital, diethyl 1,4-dihydro-2,4,6-trimethylpyridine-3, 5-dicarboxylate, and 2-allyl-2-isopropylacetamide. 5. Puromycin inhibited the induction of synthetase by pentamethylbenzene. 6. Induction of 5-aminolaevulinate synthetase correlated well with the induction of microsomal N-demethylation of p-chloro-N-methylaniline, except for phenobarbital, which induced the microsomal oxidase relatively more than the synthetase.  (+info)

The in-vitro activity of linezolid (U-100766) and tentative breakpoints. (3/1656)

The in-vitro activity of linezolid, a novel oxazolidinone, was investigated in comparison with those of amoxycillin, cefuroxime, quinupristin/dalfopristin, trovafloxacin and vancomycin against 420 recent Gram-positive and anaerobic clinical isolates. Linezolid was equally active (MIC90 1 mg/L) against methicillin-susceptible and -resistant Staphylococcus aureus. It demonstrated uniform activity against streptococci and enterococci and no cross-resistance with other agents. The time-kill kinetic data demonstrated that the in-vitro activity of linezolid was predominantly bacteriostatic; slow bactericidal activity was only observed at the higher concentration with streptococci. An increase in inoculum from 10(4) to 10(6) cfu on selected strains had little effect on the MICs (MIC90 within one dilution step) of linezolid and an increase in inoculum from 10(5) to 10(7) cfu/mL had no notable effect on the in-vitro bactericidal activity. A tentative linezolid breakpoint of 2 mg/L was chosen after analysis of distribution of susceptibilities.  (+info)

Aldehyde oxidase-dependent marked species difference in hepatic metabolism of the sedative-hypnotic, zaleplon, between monkeys and rats. (4/1656)

A marked difference in hepatic activity of aldehyde oxidase between rats and monkeys was found to be responsible for the previously reported marked species difference in the metabolism of Zaleplon in vivo. In the postmitochondrial fractions, S-9s, from liver homogenates of these animals, Zaleplon was transformed in the presence of NADPH into the side chain oxidation product, N-desethyl-Zaleplon, and the aromatic ring oxidation product, 5-oxo-Zaleplon. In the rat S-9, N-desethyl-Zaleplon and 5-oxo-Zaleplon were a major and a very minor metabolites, respectively. However, in the monkey S-9, Zaleplon was transformed into 5-oxo-Zaleplon at a much higher rate than that for N-desethyl-Zaleplon formation. N-Desethyl-Zaleplon was formed in the monkey S-9 at a rate almost equal to that in the rat S-9. N-Desethyl-5-oxo-Zaleplon was formed at a minor rate only in the monkey S-9 through N-desethyl-Zaleplon as an obligatory intermediate. The hepatic activity for the formation of 5-oxo-Zaleplon in the monkey and rat was localized in cytosol and did not require NADPH. Sensitivity to various inhibitors and requirement of water as oxygen source, using H218O, strongly suggested that the hepatic cytosolic formation of 5-oxo-Zaleplon was mediated by aldehyde oxidase. N-Desethyl-Zaleplon was formed in the presence of NADPH by microsomes from the liver of rats and monkeys, and its formation was strongly suggested using various cytochrome P-450 inhibitors to be mediated by a number of cytochrome P-450 isoforms, such as 3A, 2C, and 2D subfamilies.  (+info)

Increased transcriptional activity of prostate-specific antigen in the presence of TNP-470, an angiogenesis inhibitor. (5/1656)

Prostate-specific antigen, PSA, is regarded as a reliable surrogate marker for androgen-independent prostate cancer (AIPC). Concern has been raised that investigational agents may affect PSA secretion without altering tumour growth or volume. In a phase I trial, several patients with AIPC had elevated serum PSA levels while receiving TNP-470 that reversed upon discontinuation. TNP-470 inhibits capillary growth in several angiogenesis models. These observations prompted us to determine if TNP-470, or its metabolite, AGM-1883, altered PSA secretion. Intracellular protein and transcriptional levels of PSA and androgen receptor were also determined. The highest TNP-470 concentration produced a 40.6% decrease in cell number; AGM-1883 had minimal effects on cell viability. PSA secretion per cell was induced 1.1- to 1.5-fold following TNP-470 exposure. The same trend was observed for AGM-1883. PSA and AR were transcriptionally up-regulated within 30 min after exposure to TNP-470. PSA transcription was increased 1.4-fold, while androgen receptor (AR) transcription was induced 1.2-fold. The increased PSA transcriptional activity accounts for the increased PSA secretion. Increased AR transcription was also reflected at the protein level. In conclusion, TNP-470 and AGM-1883 both up-regulated PSA making clinical utilization of this surrogate marker problematic.  (+info)

Bcl-XL induction during terminal differentiation of friend erythroleukaemia cells correlates with delay of apoptosis and loss of proliferative capacity but not with haemoglobinization. (6/1656)

Friend murine erythroleukaemia (F-MEL) cells are a useful model for studying the processes that regulate erythroid differentiation since exposure of these cells to chemical inducers (DMSO or HMBA) results in commitment to terminal cell division and synthesis of haemoglobin. This study examined the relationship between differentiation and apoptosis in DMSO sensitive and resistant F-MEL cells. Clear apoptosis was not observed in DMSO-treated sensitive F-MEL (strain 745A) cells during the induction of differentiation. In contrast, DMSO-induced 745A cells exhibited delayed apoptosis compared to uninduced cells. Since the Bcl-2 family members play a major role in the control of apoptosis and/or differentiation, we determined their expression before and after DMSO or HMBA treatment. Neither untreated nor chemically-induced 745A cells expressed the Bcl-2 protein. The levels of Bax and Bad proteins remained relatively constant during DMSO-induced differentiation. DMSO or HMBA treatment of 745A cells induced a marked increase of Bcl-XL expression during the late phase of differentiation which persisted even when the cells began to die. This upregulation of Bcl-XL was independent of cell density but was correlated with cell arrest in G0/G1. DMSO treatment induced a similar delay of apoptosis and enhancement of Bcl-XL expression in F-MEL (strain TFP10) cells which fail to synthesize haemoglobin in the presence of DMSO. Dexamethasone, which blocks DMSO-induced differentiation of F-MEL cells, prevented the induction of Bcl-XL. Inhibitors such as imidazole or succinylacetone, which inhibit haemoglobin synthesis but not commitment to terminal cell division, did not suppress Bcl-XL induction in DMSO-induced cells. Taken together, these results indicate that DMSO treatment of F-MEL cells induces a marked increase in Bcl-XL expression suggesting a role for this anti-apoptotic protein in the process of erythroid differentiation in F-MEL cells. Moreover, induction of Bcl-XL during this process seems to be associated with loss of proliferative capacity rather than with haemoglobin synthesis.  (+info)

Activation of three types of voltage-independent Ca2+ channel in A7r5 cells by endothelin-1 as revealed by a novel Ca2+ channel blocker LOE 908. (7/1656)

1. We have shown that in addition to voltage-operated Ca2+ channel (VOC), endothelin-1 (ET-1) activates two types of Ca2+-permeable nonselective cation channel (NSCC) in A7r5 cells: its lower concentrations (< or = 1 nM; lower [ET-1]) activate only an SK&F 96365-resistant channel (NSCC-1), whereas its higher concentrations (> or = 10 nM; higher [ET-1]) activate an SK&F 96365-sensitive channel (NSCC-2) as well. 2. We now characterized the effects of a blocker of Ca2+ entry channel LOE 908 on NSCCs and store-operated Ca2+ channel (SOCC) in A7r5 cells, and using two drugs, clarified the involvement of these channels in the ET-1-induced increase in the intracellular free Ca2+ concentrations ([Ca2+]i). Whole-cell recordings and [Ca2+]i monitoring with fluo-3 were used. 3. LOE 908 up to 10 microM had no effect on increases in [Ca2+]i induced by thapsigargin or ionomycin, but SK&F 96365 abolished them. 4. In the cells clamped at -60 mV, both lower and higher [ET-1] induced inward currents with linear iv relationships and the reversal potentials of -15.0 mV. Thapsigargin induced no currents. 5. In the presence of nifedipine, lower [ET-1] induced a sustained increase in [Ca2+]i, whereas higher [ET-1] induced a transient peak and a sustained increase. The sustained increases by lower and higher [ET-1] were abolished by removal of extracellular Ca2+, and they were suppressed by LOE 908 to 0 and 35%, respectively, with the LOE 908-resistant part being abolished by SK&F 96365. 6. These results show that LOE 908 is a blocker of NSCCs without effect on SOCC, and that the increase in [Ca2+]i at lower [ET-1] results from Ca2+ entry through NSCC-1 in addition to VOC, whereas the increase at higher [ET-1] involves NSCC-1, NSCC-2 and SOCC in addition to VOC.  (+info)

Mechanisms of melatonin-induced vasoconstriction in the rat tail artery: a paradigm of weak vasoconstriction. (8/1656)

1. Vasoconstrictor effects of melatonin were examined in isolated rat tail arteries mounted either in an isometric myograph or as cannulated pressurized segments. Melatonin failed by itself to mediate observable responses but preactivation of the arteries with vasopressin (AVP) reliably uncovered vasoconstriction responses to melatonin with maxima about 50% of maximum contraction. Further experiments were conducted with AVP preactivation to 5-10% of the maximum contraction. 2. Responses to melatonin consisted of steady contractions with superimposed oscillations which were large and irregular in isometric but small in isobaric preparations. Nifedipine (0.3 microM) reduced the responses and abolished the oscillations. Charybdotoxin (30 nM) increased the magnitude of the oscillations with no change in the maximum response. 3. Forskolin (0.6 microM) pretreatment increased the responses to melatonin compared to control and sodium nitroprusside (1 microM) treated tissues. The AVP concentration required for preactivation was 10 fold higher than control in both the forskolin and nitroprusside treated groups. 4. In isometrically-mounted arteries treated with nifedipine, melatonin receptor agonists had the potency order 2-iodomelatonin > melatonin > S20098 > GR196429, and the MT2-selective antagonist luzindole antagonized the effects of melatonin with a low pK(B) of 6.1+/-0.1. 5. It is concluded that melatonin elicits contraction of the rat tail artery via an mt1 or mt1-like receptor that couples via inhibition of adenylate cyclase and opening of L-type calcium channels. Calcium channels and charybdotoxin-sensitive K channels may be recruited into the responses via myogenic activation rather than being coupled directly to the melatonin receptors. 6. It is proposed that the requirement of preactivation for overt vasoconstrictor responses to melatonin results from the low effector reserve of the melatonin receptors together with the tail artery having threshold inertia. Potentiative interactions between melatonin and other vasoconstrictor stimuli probably also result from the threshold inertia. A simple model is presented and a general framework for consideration of interactions between weak vasoconstrictor agonists and other vasoconstrictor stimuli is discussed.  (+info)

Short-term toxicity to fish: The toxicity of N,N-dimethylacetamide to fish was investigated in a static test conducted according to DIN 38412, part 15 using Leuciscus idus as test organism (BASF AG, 1979; report no. 78/277). Based on nominal test concentrations the 96-h LC50 was found to be ,500 mg/L. These data were selected as key data in terms of the chemical safety assessment. In conclusion, N,N-dimethylacetamide (CAS 127-19-5) is concluded to be with high probability acutely not harmful to fish. Long-term toxicity to fish: No experimental data available. In Annex IX section 9.1.6 of Regulation (EC) No 1907/2006, it is laid down that chronic tests shall be proposed by the registrant if the chemical safety assessment indicates the need to investigate further the effects on fish. According to Annex I of this regulation, the chemical safety assessment triggers further action when the substance or the preparation meets the criteria for classification as dangerous according to Regulation ...
The PCILO quantum-chemical method with geometry optimization has been used to study rotation barriers of methyl groups in N-methylacetamide and N,N-dimethylacetamide. In all the cases studied, the eclipsed conformation have been found to be the most stable. Cis form of N-methylacetamide is less stable than the corresponding trans form by 2.0 kJ mol-1. Moreover, the PCILO method has been used to study linear n-mers (n = 4) of N-methylacetamide. On going from the dimer to tri- and tetramers, the hydrogen-bond energies have been found non-additive, and positive cooperativity has been observed. Finally, hydrogen-bond complexes have been studied which were formed by C=O groups of N-methylacetamide and N,N-dimethylacetamide with water, methanol or phenol as proton-donors. The said proton-donors have been found to act as breakers of inter-peptide hydrogen bonds N-H...O=C. The hydrogen bonds formed by methanol are somewhat stronger than those formed by water. In accordance with experiment, the strongest ...
Read "Inhibitory effect of hexamethylene bisacetamide on replication of human cytomegalovirus, Archives of Virology" on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips.
2-(4-chloro-6-fluoro-1-indanylidene)-N-methylacetamide: an anti-inflammatory agent with both analgesic and central muscle relaxant activities; structure in first source
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As the incidence of MRSA exacerbations in CF patients increases, the need for alternative antibiotic options to that of i.v. vancomycin has become apparent. Case reports have documented successful treatment of MRSA infections with linezolid in patients with CF (12, 25, 26). It has also been evident that prolonged treatment with low doses of linezolid results in the development of resistance (13, 15). Thus, dosing regimen selection is critical in achieving a successful response while minimizing the development of resistance and adverse events. Herein, we describe the population pharmacokinetics of linezolid in eight adult CF participants using a previously described 2-compartment model with a theoretical inhibition compartment (20). This model accurately described linezolid pharmacokinetics in these participants and generally resulted in mean parameter estimates similar to those for healthy volunteers and septic shock patients, albeit with lower absolute bioavailability (20). Importantly, ...
Hydrogen bonding between |i|N, N|/i|-dimethylacetamide (DMA) and alcohols has been studied in carbon tetrachloride solution by an X-band Microwave bench at 936GHz. The dielectric relaxation time (τ) of the binary system are obtained by both Higasis method and Gopalakrishna method. The most likely association complex between alcohol and DMA is 1:1 stoichiometric complex through the hydroxyl group of the alcohol and the carbonyl group of amide. The results show that the interaction between alcohols and amides is 1:1 complex through the free hydroxyl group of the alcohol and the carbonyl group of amide and the alkyl chain-length of both the alcohols and amide plays an important role in the determination of the strength of hydrogen bond (O-H: C=O) formed and suggests that the proton donating ability of alcohols is in the order: 1-propanol < 1-butanol < 1-pentanol and the accepting ability of DMA.
Lacosamide is used in the treatment of seizures.get complete information about lacosamide including usage, side effects, drug interaction, expert advice along with medicines associated with lacosamide at 1mg.com
Abstract: Thermal and electrochemical properties of new low-temperature molten salt electrolytes based on LiClO4 with acetamide or ethyleneurea have been studied by differential scanning calorimetry, ac impedance spectroscopy and cyclic voltammertry, respectively. These electrolytes appear as liquid at room temperature through they are composed of two solids. DSC analysis shows that the LiClO4-acetamide electrolyte has the preferable thermal stability. The conductivity of LiClO4-acetamide electrolyte with a molar ratio of 1.0:5.5 is 1.25×10-3 S•cm-1 at 25 ℃ and 1.15×10-2 S•cm-1 at 80 ℃,and the electrochemical window of it is about 3 V. Key words: Molten salt electrolytes, Thermal properties, Ionic conductivity, Lithium perchlorate, Acetamide, Ethyleneurea ...
N-[2-(5-methoxy-2-phenyl-1H-indol-3-yl)ethyl]acetamide chemical properties, What are the chemical properties of N-[2-(5-methoxy-2-phenyl-1H-indol-3-yl)ethyl]acetamide 151889-03-1, What are the physical properties of N-[2-(5-methoxy-2-phenyl-1H-indol-3-yl)ethyl]acetamide ect.
N-[2-(pyrrol-1-ylamino)phenyl]acetamide 87948-01-4 NMR spectrum, N-[2-(pyrrol-1-ylamino)phenyl]acetamide H-NMR spectral analysis, N-[2-(pyrrol-1-ylamino)phenyl]acetamide C-NMR spectral analysis ect.
Acetamide has been detected near the center of the Milky Way galaxy.[5] This finding is potentially significant because acetamide has an amide bond, similar to the essential bond between amino acids in proteins. This finding lends support to the theory that organic molecules that can lead to life (as we know it on Earth) can form in space. In addition, acetamide is found infrequently on burning coal dumps, as a mineral of the same name.[6][7] ...
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This is a one-period, double-blind, single-center pharmacokinetic study of linezolid in patients with MDR or XDR tuberculosis treated with linezolid and an Optimized Background Therapy (defined as treatment with , 4 drugs with activity against tuberculosis to which the patients isolate is believed to be sensitive by history or based on drug sensitivity testing ...
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Agents that trigger cell differentiation are highly efficacious in treating certain cancers, but such approaches are not generally effective in most malignancies. Compounds such as DMSO and hexamethylene bisacetamide (HMBA) have been used to induce differentiation in experimental systems, but their mechanisms of action and potential range of uses on that basis have not been developed. Here, we show that HMBA, a compound first tested in the oncology clinic over 25 years ago, acts as a selective bromodomain inhibitor. Biochemical and structural studies revealed an affinity of HMBA for the second bromodomain of BET proteins. Accordingly, both HMBA and the prototype BET inhibitor JQ1 induced differentiation of mouse erythroleukemia cells. As expected of a BET inhibitor, HMBA displaced BET proteins from chromatin, caused massive transcriptional changes, and triggered cell-cycle arrest and apoptosis in Myc-induced B-cell lymphoma cells. Furthermore, HMBA exerted anticancer effects in vivo in mouse ...
Lacosamide is an anticonvulsant used either alone or in a combination with other medicines for the treatment of seizures. The oral forms of this medicine are not recommended for use in patients less than 4 years of age. The injectable form of this medicine is not recommended for use in patients less than 17 years of age. Buy Lacosamide Online. Know uses, side effects, dosage, contraindications, substitutes, benefit, interactions, purpose, drug interactions, precautions, warnings etc. Download Practo app & get your medicines home delivered.
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Substituted 2-arylacetamides are very interesting compounds because of their structural similarity to the lateral chain of natural benzyl penicillin (Mijin et al., 2006, 2008). Amides are also used as ligands due to their excellent coordination abilities (Wu et al., 2008, 2010). The room temperature crystal structure of the title compound was reported without hydrogen atom coordinates in the orthorhombic space group Pna21 (Andreetti et al., 1968). We report herein on the crystal structure of the monoclinic polymorph that crystallized in space group P21/c.. The molecular structure of the title compound is illustrated in Fig. 1. Bond lengths are in normal ranges (Allen et al., 1987) but show slight changes from those reported for some similar acetamide derivatives viz., N-(4-chloro-1,3-benzothiazol-2-yl)-2-(3-methylphenyl)acetamide monohydrate (Praveen et al., 2011a), N-(3-chloro-4-fluorophenyl)-2,2-diphenylacetamide (Praveen et al., 2011b) and ...
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You are viewing an interactive 3D depiction of the molecule 2-bromo-n-{(1e,4e)-3-methyl-4-[(phenylsulfonyl)imino]-2,5-cyclohexadien-1-ylidene}acetamide (C15H13BrN2O3S) from the PQR.
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N-(2-(4-t-butylbenzyl)-3-(pivaloyloxy)propyl)-2-(3-fluoro-4-(methylsulfonylamino)phenyl)propionamide: a TRPV1 antagonist; structure in first source
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Crystallise the acetamide repeatedly from absolute EtOH, EtOAc (m 160-161o) or H2O (m 159-160o). Dry it in vacuo over P2O5. [Beilstein 9 H 347, 9 III 2193, 9 IV 1632 ...
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Murine erythroleukemia cells (MELC) are transformed cells that can be induced to differentiate by a variety of agents, such as hexamethylenebisacetamide (HMBA) and dimethyl sulfoxide. Dexamethasone suppresses HMBA-mediated MELC differentiation, but MELC retain a memory for their exposure to HMBA since, on transfer from culture with HMBA and dexamethasone to medium without additions, a portion of the cells express characteristics of terminal differentiation. This study characterizes the steroid suppressed steps in the multi-step process of inducer-mediated MELC terminal differentiation. MELC in culture with HMBA and dexamethasone show low levels of commitment to terminal cell division; upon transfer to culture with inducer alone there is a rapid increase in the proportion of committed cells. The magnitude of this rapid or "step-up" expression of commitment increased with the length of prior culture with inducer and steroid. This step-up expression is not inhibited by actinomycin D or cordycepin ...
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... pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO)". Bioorg. ... pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands". Bioorg. Med. Chem. 9 (10): ...
... alkylamino acetamides as orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 18 (20): 5420-3. doi:10.1016 ... alkylamino acetamides Compound 1m - Selective OX2 antagonist Orexin receptor GRCh38: Ensembl release 89: ENSG00000137252 - ...
It also reacts with alcohols and amines to produce acetate esters and acetamides, respectively. Acetyl bromide[permanent dead ...
These ligands afford a very active and productive catalyst, which efficiently reduces a various acetamides. It is worth noting ...
... acetamides: selective dopamine D4 receptor agonists". Bioorganic & Medicinal Chemistry. 12 (13): 3471-83. doi:10.1016/j.bmc. ...
... pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO)". Bioorg. ...
... acetamides as Probes of Mitochondrial Steroidogenesis - A New Mechanism for GABAA Receptor Modulation. Angew. Chem. Int. Ed. ...
... of thioacetic acid such as potassium thioacetate can be used to do one-step conversion of aryl nitrates to aryl acetamides. ...
... acetamides MeSH D02.241.081.038.108.080 --- 2-acetylaminofluorene MeSH D02.241.081.038.108.080.070 --- ...
Alpha Aryl Acetamides) Über Benzimidazolderivate mit starker analgetischer Wirkung - CELLULAR AND MOLECULAR LIFE SCIENCES CMLS ...
2012). "Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate ...
... acetamides" (in German), J. Org. Chem. 38 (23): pp. 4073-4074, doi:10.1021/jo00987a029 "1-Phenylnaphthalene". Organic Syntheses ...
InChI=1S/C26H32N4O4S/c1-20(2)30(16-10-11-17-34-19-24(31)29-35(3,32)33)23-18-27-25(21-12-6-4-7-13-21)26(28-23)22-14-8-5-9-15-22/h4-9,12-15,18,20H,10-11,16-17,19H2,1-3H3,(H,29,31) ...
Acetamides. Hidden categories: *Drugs with non-standard legal status. *Articles without EBI source ...
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InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16-,19+,22+,23-,24+,27+/m0/s1 ...
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Palladium-catalyzed C-H acetoxylation reactions of 2-methoxyimino-2-aryl-acetates and acetamides have been developed. These ... Palladium-catalyzed C-H acetoxylation of 2-methoxyimino-2-aryl-acetates and acetamides L. Wang, X. Xia, W. Guo, J. Chen and W. ... acetamides. have been developed. These transformations feature excellent regioselectivity, wide substrate scope, and moderate ... Palladium-catalyzed C-H acetoxylation of 2-methoxyimino-2-aryl-acetates and acetamides ...
Pages in category "Acetamides". The following 23 pages are in this category, out of 23 total. This list may not reflect recent ... The following are the current most viewed articles on Wikipedia within Wikipedias Acetamides category. Think of it as a Whats ... Hot list for Acetamides. More info ». This is a beta release and so the figures may be a day or two out of date. Wed love to ...
Design, Synthesis and Anticancer Evaluation of Acetamides Comprising 1,2,3-triazole, 1,3,4-thiadiazole and Isothiazolo[4,3-b] ... Title:Design, Synthesis and Anticancer Evaluation of Acetamides Comprising 1,2,3-triazole, 1,3,4-thiadiazole and Isothiazolo[4, ... Synthesis and Anticancer Evaluation of Acetamides Comprising 1,2,3-triazole, 1,3,4-thiadiazole and Isothiazolo[4,3-b]pyridine ...
2-chloro-N-(5-aryl-1,3-thiazol-2-yl)acetamides 3a-h have been prepared in good yields] by the reaction of 2-amino-5-(R-benzyl) ... Synthesis and antitumor activities of new n-(5-benzylthiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides. Biopolym. Cell. 2018, ... Synthesis of series of new N-(5-benzyl-thiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides and study on their anticancer activity ... Synthesis and antitumor activities of new n-(5-benzylthiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides ...
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Catalytic Enantioselective Conjugate Addition of Azaarylacetates and Acetamides to Nitroalkenes An enantioselective nickel- ... catalysed Michael addition of azaarylacetates and acetamides to nitroalkenes has been developed. A range of azaaryl ... allylation of alkylidene malonates and enantioselective nickel-catalysed Michael additions of azaarylacetates and acetamides to ...
... alkyl acetamides such as, for example, dimethyl acetamide and dimethyl formamide; sulfoxides such as for example, dimethyl ... acetamides; sulfoxides; sulfones; pyrrolidones; oxa acids; diglycolic acids; and any analogs, derivatives, copolymers and ...
Phenyl Acetamides. US20090050526 *. Sep 18, 2008. Feb 26, 2009. Kaidong Chen. Process for Recycling an Active Slurry Catalyst ...
... pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO)". Bioorg. ... pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands". Bioorg. Med. Chem. 9 (10): ...
acetamide (plural acetamides). *(organic chemistry) The amide of acetic acid, CH3CONH2. ...
Acetamides [‎2]‎. Acetaminophen [‎5]‎. Acetic Acid [‎1]‎. Acetylcarnitine [‎1]‎. Acetylcholinesterase [‎1]‎. Acquired ...
Diphenamid (acetamides). Flufenacet (oxyacetamides). Fentrazamide (tetrazolinones). Mitosis inhibitors (K3(15)). Bensulfuron- ...
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Acetamides / pharmacokinetics * Acetamides / therapeutic use * Anti-Bacterial Agents / pharmacokinetics* * Anti-Bacterial ...
Acetamides / pharmacology * Animals * Cell Transformation, Neoplastic* * Endothelial Growth Factors / isolation & purification ...
... alkylamino acetamides as orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 18 (20): 5420-3. doi:10.1016 ... alkylamino acetamides Compound 1m - Selective OX2 antagonist Orexin receptor GRCh38: Ensembl release 89: ENSG00000137252 - ...
1. Indole-3-acetamides.. Dillard RD, Bach NJ, Draheim SE, Berry DR, Carlson DG, Chirgadze NY, Clawson DK, Hartley LW, Johnson ...
2-[[5-(Substituted-phenyl]-1,3,4-oxadiazol-2-yl]sulfanyl]-N-[1,3-thiazol-2-yl]acetamides: new bi-heterocycles as possible ... 2-[[5-(Substituted-phenyl]-1,3,4-oxadiazol-2-yl]sulfanyl]-N-[1,3-thiazol-2-yl]acetamides: ...
In this work, a new series of 2-[4-[2-furoyl]-1-piperazinyl]-N-aryl/aralkyl acetamides has been synthesized and evaluated for ... Synthesis of some new 2-[4-[2-furoyl]-1-piperazinyl]-N-aryl/aralkyl acetamides as potent antibacterial agents ... Synthesis of some new 2-[4-[2-furoyl]-1-piperazinyl]-N-aryl/aralkyl acetamides as potent a ... N-aryl/aralkyl acetamides [5a-u]. The structural elucidation was done by EI-MS, IR and 1 H-NMR techniques of all the ...
Biotransformations of nitro-aromatic compounds to amines and acetamides by tuberous roots of Arracacia xanthorrhiza and Beta ... Biotransformations of nitro-aromatic compounds to amines and acetamides by tuberous roots of Arracacia xanthorrhiza and Beta ... Biotransformations of nitro-aromatic compounds to amines and acetamides by tuberous roots of Arracacia xanthorrhiza and Beta ... Biotransformations of nitro-aromatic compounds to amines and acetamides by tuberous roots of Arracacia xanthorrhiza and Beta ...
Chowdary, PVR and Raveendran, N and Ali, Hina (2013) Rational Design and Synthesis of Some Novel Substituted Acetamides Bearing ... Rational Design and Synthesis of Some Novel Substituted Acetamides Bearing 2-[3-acetyl-(1hindol- 1-yl/5-methoxy-1h-indol-1-yl ... So some new compounds, substituted acetamides bearing indole moiety which are related to rivastigmine were designed and ... 2 -chlorocycloaminoethanones and 2- chloro N- alkyl acetamides were synthesized by adding chloroacetyl chloride dropwise to a ...
The synthesis of 4-thiazolidinone derivatives using 2-(4-R-2-formylphenoxy)-N-(R-phenyl)acetamides and their anti-inflammatory ... 4-thiazolidinones; NSAIDs; 2-(4-R-2-formylphenoxy)-N-(R-phenyl)acetamides; anti-exudative activity ... acetamides has been synthesized from salicylic aldehydes for structural modifications of basic heterocycles. The aldehydes ...
The synthesis of 4-thiazolidinone derivatives using 2-(4-R-2-formylphenoxy)-N-(R-phenyl)acetamides and their anti-inflammatory activity
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  • So some new compounds, substituted acetamides bearing indole moiety which are related to rivastigmine were designed and synthesized. (manipal.edu)
  • These compounds were then derivatized by N-acylation of the 11- and 17-imine nitrogens with chloroacetyl chloride and the resulting chloroacetamides were then condensed with 2-hydroxy-1-napthaldehyde in Darzens-type reactions forming the corresponding epoxy acetamides in the side chains. (ovid.com)
  • In addition, a number of aryl alkyl acetamides were derivatized with the same chiral isocyanate and the preliminary results of the NMR and chromatographic properties of the derived diastereomeric ureides is presented. (illinois.edu)
  • Growth regulators and acetamides are the herbicides most commonly associated with twisted whorls or "buggy-whipping. (pioneer.com)
  • Synthesis of series of new N-(5-benzyl-thiazol-2-yl)-2-(heteryl-5-ylsulfanyl)-acetamides and study on their anticancer activity. (enamine.net)
  • Design and synthesis of -phenoxy-N-sulfonylphenyl acetamides as Trypanosoma brucei leucyl-tRNA synthetase inhibitors. (elsevier.com)
  • It is also used as a reactant for synthesis of 3-substituted 2-indolinone RET kinase inhibitors and for preparation of indolone acetamides as antiseizure agents. (alfa.com)
  • V. Kanagarajan, J. Thanusu, and M. Gopalakrishnan, "Synthesis and in vitro microbiological evaluation of an array of biolabile 2-morpholino- N -(4,6-diarylpyrimidin-2-yl)acetamides," European Journal of Medicinal Chemistry , vol. 45, no. 4, pp. 1583-1589, 2010. (hindawi.com)
  • Synthesis and in-vitro inotropic evaluation of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,riazolo[4,3-a]quinolin-7-yl)acetamides. (biomedsearch.com)
  • We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,riazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. (biomedsearch.com)
  • Furthermore, reaction of the (1H-imidazol-1-yl)acetates with primary amines yielded the corresponding acetamides. (uzh.ch)
  • An effective and robust iridium pincer complex achieves a selective α-alkylation of tertiary and secondary acetamides involving a borrowing hydrogen methodology. (organic-chemistry.org)
  • The new derivatives were prepared by condensation of the 4-en-3-one moiety of the four steroids with 2-hydroxy-1-naphthaldehyde to afford a series of 4-(R)-hydroxy-(2-hydroxynaphtalen-1-yl) adducts. (ovid.com)
  • An efficient and general palladium-catalyzed intramolecular aminoalkylation of alkenyl aromatic α-halo acetamides with a wide substrate scope under mild conditions has been developed, yielding diverse dihydropyrroloindole derivatives of pharmaceutical interest. (hku.hk)
  • Discovery of indolone acetamides as novel SV2A ligands with improved potency toward seizure suppression. (alfa.com)
  • Activity of 2-(quinolin-4-yloxy)acetamides in Mycobacterium tuberculosis clinical isolates and identification of their molecular target by whole-genome sequencing. (pubfacts.com)
  • The following are the current most viewed articles on Wikipedia within Wikipedia's Acetamides category. (thefullwiki.org)
  • Catalytic Enantioselective Conjugate Addition of Azaarylacetates and Acetamides to Nitroalkenes An enantioselective nickel-catalysed Michael addition of azaarylacetates and acetamides to nitroalkenes has been developed. (ed.ac.uk)