Category: Pyrazines

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Drug Metabolism and Disposition called Utility of MetaSite in improving metabolic stability of the neutral indomethacin amide derivative and selective cyclooxygenase-2 inhibitor 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-N-phenethyl-acetamide, Author is Boyer, David; Bauman, Jonathan N.; Walker, Daniel P.; Kapinos, Brendon; Karki, Kapil; Kalgutkar, Amit S., which mentions a compound: 1827-27-6, SMILESS is NC1=CN=C(C=C1)F, Molecular C5H5FN2, Electric Literature of C5H5FN2.

Prediction of the metabolic sites for new compounds, synthesized or virtual, is important in the rational design of compounds with increased resistance to metabolism The aim of the present investigation was to use rational design together with MetaSite, an in silico tool for predicting metabolic soft spots, to synthesize compounds that retain their pharmacol. effects but are metabolically more stable in the presence of cytochrome P 450 enzymes. The model compound for these studies was the phenethyl amide (1) derivative of the nonsteroidal anti-inflammatory drug (NSAID) indomethacin. Unlike the parent NSAID, 1 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor and nonulcerogenic anti-inflammatory agent in the rat. This pharmacol. benefit is offset by the finding that 1 is very unstable in rat and human microsomes because of extensive P 4503 A4/2D6-mediated metabolism on the phenethyl group, exptl. observations that were accurately predicted by MetaSite. The information was used to design analogs with polar (glycinyl) and/or electron-deficient (fluorophenyl, fluoropyridinyl) amide substituents to reduce metabolism in 1. MetaSite correctly predicted the metabolic shift from oxidation on the amide substituent to O-demethylation for these compounds, whereas rat and human microsomal stability studies and pharmacokinetic assessments in the rat confirmed that the design tactics for improving pharmacokinetic attributes of 1 had worked in our favor. In addition, the fluorophenyl and pyridinyl amide derivatives retained the potent and selective COX-2 inhibition demonstrated with 1. Overall, the predictions from MetaSite gave useful information leading to the design of new compounds with improved metabolic properties.

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Yu, Bin; Zhao, Bin; Hao, Zesheng; Chen, Lei; Cao, Lixin; Guo, Xiaofeng; Zhang, Nailou; Yang, Dongyan; Tang, Liangfu; Fan, Zhijin published the article 《Design, synthesis and biological evaluation of pyrazole-aromatic containing carboxamides as potent SDH inhibitors》. Keywords: pyrazole thiazole aryl carboxamide preparation antifungal SDH inhibitor SAR; Antifungal activity; Molecular docking; Structure-activity relationships; Succinate dehydrogenase inhibitors.They researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Category: pyrazines. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:591-54-8) here.

To continue studies on discovery of new potent antifungal leads, 43 novel pyrazole-aromatic containing carboxamides were rationally designed and synthesized. Bioassays indicated that most target compounds displayed good in vitro antifungal activities against Botrytis cinerea, Rhizoctonia cerealis and Sclerotinia sclerotiorum and in vivo antifungal activity against R. solani. Compound I exhibited the most significant in vitro activity against R. cerealis (EC50 = 0.93μg/mL) with about 2-fold more potent than a previously reported lead compound N-(3-bromophenyl)-2-[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]-4-thiazolecarboxamide (EC50 = 2.01μg/mL), and about 11-fold more potent than the pos. control/com. succinate dehydrogenase inhibitor thifluzamide (EC50 = 23.09μg/mL). Structure-activity relationship anal. and mol. docking simulations indicated that the presence of difluoromethyl pyrazole-(m-benzene)carboxamide scaffold obviously increased the antifungal activity. The further enzymic bioassay showed that both thifluzamide and compound I displayed excellent SDH inhibitory effects, and fluorescence quenching anal. suggested that they may share the same target SDH.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Development of highly sensitive fluorescent assays for fatty acid amide hydrolase, the main research direction is fluorescent assay fatty acid amide hydrolase human liver microsome; fluorometry.Recommanded Product: 5-Amino-2-fluoropyridine.

Fatty acid amide hydrolase (FAAH) is a pharmaceutical target whose inhibition may lead to valuable therapeutics. Sensitive substrates for high-throughput assays are crucial for the rapid-screening FAAH inhibitors. Here we describe the development of novel and highly sensitive fluorescent assays for FAAH based on substituted aminopyridines. Examining the relationship between the structure and the fluorescence of substituted aminopyridines suggested that a methoxy group in the para position relative to the amino group in aminopyridines greatly increased the fluorescence (i.e., quantum yields approach unity). These novel fluorescent reporters had a high Stokes’ shift of 94 nm, and their fluorescence in buffer systems increased with pH values from neutral to basic. Fluorescent substrates with these reporters displayed a very low fluorescent background and high aqueous solubility Most importantly, fluorescent assays for FAAH based on these substrates were at least 25 times more sensitive than assays using related compounds with published colorimetric or fluorescent reporters. This property results in shorter assay times and decreased protein concentrations in the assays. Such sensitive assays will facilitate distinguishing the relative potency of powerful inhibitors of FAAH. When these fluorescent substrates were applied to human liver microsomes, results suggested that there was at least one amide hydrolase in addition to FAAH that could hydrolyze long-chain fatty acid amides. These results show that these fluorescent substrates are very valuable tools in FAAH activity assays including screening inhibitors by high-throughput assays instead of using the costly and labor-intensive radioactive ligands. Potential applications of novel fluorescent reporters are discussed.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Sather, Aaron C.; Martinot, Theodore A. researched the compound: 4-Bromo-1-methyl-2-nitro-1H-imidazole( cas:121816-79-3 ).Recommanded Product: 121816-79-3.They published the article 《Data-Rich Experimentation Enables Palladium-Catalyzed Couplings of Piperidines and Five-Membered (Hetero)aromatic Electrophiles》 about this compound( cas:121816-79-3 ) in Organic Process Research & Development. Keywords: data experimentation palladium catalyzed coupling piperidine heterocyclic electrophile. We’ll tell you more about this compound (cas:121816-79-3).

To circumvent a current limitation in palladium-catalyzed C-N cross-coupling methodol., high-throughput experimentation was used to identify a catalyst capable of fusing piperidine-based nucleophiles with five-membered (hetero)aromatic bromides. A decomposition pathway for the standard electrophile was found, and a base screen was used to identify conditions that suppress this undesired transformation. Building on this, systematic optimization using a Design of Experiments approach delivered mild reaction conditions that were then subsequently applied to a variety of coupling partners.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 2150-55-2, is researched, Molecular C4H6N2O2S, about The analysis of 2-amino-2-thiazoline-4-carboxylic acid in the plasma of smokers and non-smokers, the main research direction is forensic analysis ATCA plasma human smoker GC MS; cyanide poisoning biomarker ACTA plasma human smoker GC MS; gas chromatog mass spectrometry ACTA plasma human cyanide poisoning.Application In Synthesis of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

ATCA (2-amino-2-thiazoline-4-carboxylic acid) is a promising marker to assess cyanide exposure because of several advantages of ATCA anal. over direct determination of cyanide and alternative cyanide biomarkers (i.e. stability in biol. matrixes, consistent recovery, and relatively small endogenous concentrations). Concentrations of ATCA in the plasma of smoking and nonsmoking human volunteers were analyzed using gas chromatog. mass spectrometry to establish the feasibility of using ATCA as a marker for cyanide exposure. The levels of ATCA in plasma of smoking volunteers, 17.2 ng/mL, were found to be significantly (p < 0.001) higher than that of nonsmoking volunteers, 11.8 ng/mL. Comparison of ATCA concentrations of smokers relative to nonsmokers in both urine and plasma yielded relatively similar results. The concentration ratio of ATCA for smokers vs. nonsmokers in plasma and urine was compared to similar literature studies of cyanide and thiocyanate, and correlations are discussed. This study supports previous evidence that ATCA can be used to determine past cyanide exposure and indicates that further studies should be pursued to validate the use of ATCA as a marker of cyanide exposure. As far as I know, this compound(2150-55-2)Application In Synthesis of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

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Pyrazine – Wikipedia,
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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Aminopyrimidine(SMILESS: C1=CN=CN=C1N,cas:591-54-8) is researched.Application In Synthesis of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. The article 《Spectrum of antiviral activity of 4-aminopyrimidine N-oxides against a broad panel of tick-borne encephalitis virus strains》 in relation to this compound, is published in Antiviral Chemistry and Chemotherapy. Let’s take a look at the latest research on this compound (cas:591-54-8).

Tick-borne encephalitis is an important human arbovirus neuroinfection spread across the Northern Eurasia. Inhibitors of tick-borne encephalitis virus (TBEV) strain Absettarov, presumably targeting E protein n-octyl-β-D-glucoside (β-OG) pocket, were reported earlier. In this work, these inhibitors were tested in vitro against seven strains representing three main TBEV subtypes. The most potent compound, 2-[(2-methyl-1-oxido-5,6,7,8-tetrahydroquinazolin-4-yl)amino]-phenol, showed EC50 values lower than 22 μM against all the tested strains. Nevertheless, EC50 values for virus samples of certain strains demonstrated a substantial variation, which appeared to be consistent with the presence of E protein not only in infectious virions, but also in non-infectious and immature virus particles, protein aggregates, and membrane complexes.

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Application of 2150-55-2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Kinetic properties of a L-cysteine desulfhydrase-deficient mutant in the enzymic formation of L-cysteine from D,L-ATC.

A mutant strain lacking L-cysteine desulfhydrase was screened after UV treatment of Pseudomonas sp. CU6. The properties of the original and mutant strains were compared on the basis of parameter values estimated from kinetic simulation of the enzymic formation of L-cysteine from D,L-2-amino-Δ2-thiazoline-4-carboxylic acid (ATC). Both strains suffered from product inhibition, but inhibition was less for the mutant strain.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Detoxication of cyanide by cystine, published in 1956, which mentions a compound: 2150-55-2, Name is 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, Molecular C4H6N2O2S, Synthetic Route of C4H6N2O2S.

cf. C.A. 46, 5633a. Chem. studies on the nature of the reaction product between cystine and cyanide support formulation of the structure as 2-imino-4-thiazolidinecarboxylic acid (I). I was inert metabolically when fed to the rat or injected. I with acid yielded a small amount of thiocyanate. I was isolated from the urine of rats given NaCN subcutaneously; 80% of the cyanide was accounted for as thiocyanate. When L-cystine-S35 was administered 1st, the compounds excreted were labeled. Radioactivity measurements showed that I came from cystine, while the thiocyanate was formed from other sources of S. The reaction with cystine constitutes an independent pathway for detoxification of cyanide. The method of Schöberl and Hamm (C.A. 43, 1014f) yielded 66% I, m. 212°, [α]D29 -2.18° (c 1, water). I with Raney Ni yielded alanine. I with Ac2O in alk. aqueous solution yielded the 3-Ac compound (II), m. 179-80°, [α]D29 -1.52° (c 1, water). I (5 g.) in EtOH saturated with dry HCl and allowed to stand 24 hrs. yielded 5 g. Et ester-HCl, m. 115-16°. The Et ester of II, m. 136°.

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Huai, Lihua; Chen, Ning; Yang, Wenbo; Bai, Gang published the article 《Metabolic control analysis of L-cysteine producing strain TS1138 of Pseudomonas sp》. Keywords: model cysteine Pseudomonas metabolic control analysis.They researched the compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2 ).Application In Synthesis of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:2150-55-2) here.

A kinetic model describing the biosynthesis of L-cysteine by Pseudomonas sp. TS1138 has been developed. The two enzymes catalyzing this pathway, L-cysteine synthetase (CS) and L-cysteine desulfhydrase (CD), follow Michaelis-Menten kinetics with noncompetitive inhibition of CS by L-cysteine. From measurements of intermediates and end products that were made during L-cysteine enzymic synthesis, metabolic control anal. of the pathway was carried out using the kinetic model. The elasticity coefficients and the flux control coefficients were calculated, and the anal. revealed a shift in the flux control from CS to CD during the reaction. The findings further implicate potential targets and strategies for increasing L-cysteine production; for example, the strain TS1138 could be manipulated by site-directed mutagenesis to reduce CD activity.

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Pyrazine – Wikipedia,
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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Wang, Pu; Yin, Jiangfeng; He, Junyao; Liang, Fayong researched the compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2 ).Synthetic Route of C4H6N2O2S.They published the article 《Enzymatic syntheses of L-cysteine by sodium alginate/gelatin co-immobilized Pseudomonas sp. B-3》 about this compound( cas:2150-55-2 ) in Zhongguo Shipin Xuebao. Keywords: Pseudomonas cysteine sodium alginate gelatin immobilization fermentation. We’ll tell you more about this compound (cas:2150-55-2).

The immobilization of Pseudomonas sp. B-3 by sodium alginate/gelatin mixed gel and the biosynthesis of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) by immobilized cells were investigated. Suitable method for the immobilization of Pseudomonas sp. B-3 was selected by the comparison of eight immobilization methods. The influences of some key factors such as gel constitution, cells embedded and activation time on enzyme activity were optimized. Tween-60, N-carbamyl-L-cysteine amidohydrolase (L-NCC hydrolase) activator of Mn2+ and L-cysteine desulfhydrase inhibitor of hydroxylamine was added into reaction solution to improve L-cysteine productivity. Sodium alginate/gelatin co-immobilization showed both the highest enzyme activity and best gel strength. After 10 h activation for immobilized cells, the bioconversion was conducted at pH 8.0 and 42° for 10 h, 9.18 g/L-1 of L-cysteine was formed from 20 g/L-1 of DL-ATC/3H2O, with the molar conversion rate of 75.83%. An increase of 29.0% for L-cysteine production was obtained after catalyzed by immobilized cells in comparison with resting cells. After reused for four times, the relative molar conversion rate of L-cysteine remained 71.5% of the initial value. Sodium alginate/gelatin embedding method was suitable for immobilization of Pseudomonas sp. B-3. L-cysteine production was enhanced by the addition of Tween-60, Mn2+ and hydroxylamine hydrochloride in reaction solution

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem