Month: April 2022

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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Pyrazine – Wikipedia,
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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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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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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 1827-27-6, is researched, SMILESS is NC1=CN=C(C=C1)F, Molecular C5H5FN2Journal, Article, Archiv der Pharmazie (Weinheim, Germany) called Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides, Author is Demjen, Andras; Alfoeldi, Robert; Angyal, Aniko; Gyuris, Mario; Hackler, Laszlo Jr.; Szebeni, Gabor J.; Woelfling, Janos; Puskas, Laszlo G.; Kanizsai, Ivan, the main research direction is imidazopyrazolecarboxamide preparation antitumor breast leukemia structure activity; Groebke-Blackburn-Bienaymé reaction; anticancer agents; cytotoxic; imidazo[1,2-b]pyrazole; multicomponent reaction.Application of 1827-27-6.

The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2-b]pyrazole-7-carboxamides were investigated. Following a hit-to-lead optimization exploiting 2D and 3D cultures of MCF-7 human breast, 4T1 mammary gland, and HL-60 human promyelocytic leukemia cancer cell lines, a 67-membered library was constructed and the structure-activity relationship (SAR) was determined Seven synthesized analogs exhibited sub-micromolar activities, from which compound 63 (2-(tert-Butyl)-N-(4-fluorophenyl)-3-((2,4,4-trimethylpentan-2-yl)amino)-1H-imidazo[1,2-b]pyrazole-7-carboxamide) exerted the most significant potency with a remarkable HL-60 sensitivity (IC50 = 0.183 μM).

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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 Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin, published in 2020-05-14, which mentions a compound: 591-54-8, Name is 4-Aminopyrimidine, Molecular C4H5N3, Category: pyrazines.

Apcin is one of the few compounds that have been previously reported as a Cdc20 specific inhibitor, although Cdc20 is a very promising drug target. We reported here the design, synthesis, and biol. evaluations of 2,2,2-trichloro-1-aryl carbamate derivatives as Cdc20 inhibitors. Among these derivatives, compound 9f(I) was much more efficient than the pos. compound apcin in inhibiting cancer cell growth, but it had approx. the same binding affinity with apcin in SPR assays. It is possible that another mechanism of action might exist. Further evidence demonstrated that compound 9f also inhibited tubulin polymerization, disorganized the microtubule network, and blocked the cell cycle at the M phase with changes in the expression of cyclins. Thus, it induced apoptosis through the activation of caspase-3 and PARP. In addition, compound 9f inhibited cell migration and invasion in a concentration-dependent manner. These results provide guidance for developing the current series as potential new anticancer therapeutics.

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Pyrazine – Wikipedia,
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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 2150-55-2, is researched, SMILESS is O=C(C1N=C(N)SC1)O, Molecular C4H6N2O2SJournal, Article, Bioscience, Biotechnology, and Biochemistry called N-carbamoyl-L-cysteine as an intermediate in the bioconversion from D,L-2-amino-Δ2-thiazoline-4-carboxylic acid to L-cysteine by Pseudomonas sp. ON-4a, Author is Tamura, Yoshiharu; Nishino, Mizuka; Ohmachi, Tetsuo; Asada, Yoshihiro, the main research direction is Pseudomonas carbamoylcysteine; 2-amino-Δ 2-thiazoline-4-carboxylic acid (ATC); L-cysteine; N-carbamoyl-L-cysteine (L-NCC); Pseudomonas species; bioconversion.Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

The authors investigated the conversion of D,L-2-amino-Δ2-thiazoline-4-carboxylic (D,L-ATC) to L-cysteine with Pseudomonas sp. ON-4a, an ATC-assimilating bacterium. Cysteine and N-carbamoylcysteine (NCC), but not S-carbamoylcysteine (SCC), were produced from D,L-ATC by a cell-free extract from the strain. These products were isolated from the reaction mixture and then identified as the L-form. Similar results were obtained with P. putida AJ3865 and unidentified strain TG-3, an ATC-assimilating bacteria. It became clear that L-NCC is an intermediate in the conversion of D,L-ATC to L-cysteine in these Pseudomonas strains. Furthermore, it was suggested that these bacteria have L-ATC hydrolase and L-NCC amidohydrolase.

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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: Ethyl oxazole-5-carboxylate(SMILESS: O=C(C1=CN=CO1)OCC,cas:118994-89-1) is researched.Safety of 4-Bromo-1-methyl-2-nitro-1H-imidazole. The article 《Visible-Light Photoredox-Catalyzed Decarboxylative Alkylation of Heteroarenes Using Carboxylic Acids with Hydrogen Release》 in relation to this compound, is published in Organic Letters. Let’s take a look at the latest research on this compound (cas:118994-89-1).

Herein, we have developed visible-light photoredox-catalyzed decarboxylating carboxylic acids for alkylation of heteroarenes under mild conditions. The transformation occurred smoothly without the requirement of stoichiometric oxidants in the presence of 0.3 equiv of base, which benefited from the release of hydrogen (H2) and carbon dioxide (CO2). Various substrates and functional groups were tolerated. Primary mechanistic studies suggest that an oxidative quenching pathway and a reductive quenching pathway are both possible in the catalytic cycle.

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Safety of 4-Bromo-1-methyl-2-nitro-1H-imidazole. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 4-Bromo-1-methyl-2-nitro-1H-imidazole, is researched, Molecular C4H4BrN3O2, CAS is 121816-79-3, about Synthesis and reactions of brominated 2-nitroimidazoles. Author is Palmer, Brian D.; Denny, William A..

Imidazoles reacted with N-bromosuccinimide to give 4-bromo derivatives I (R1 = H, Me, CPh3; R2 = H, NO2, Me). 2-Nitroimidazole gave dibromo compound II as the only product. I (R1 = CPh3, R2 = H) was treated with BuLi, PrONO2, and HCl to give I (R1 = H, R2 = NO2).

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Synthetic studies on bengazoles of marine sponge origin. Synthesis of the core bis-oxazole fragments.Reference of Ethyl oxazole-5-carboxylate.

The core bis-oxazole fragment I (R = OCH2OMe, R1 = CHO) was constructed by the coupling of 5-formyloxazole with lithiated 5-(silyoxymethyl)oxazoles, oxidation of the resulting bis(oxazolyl)methanol (II), followed by the asym. reduction with (R)-(+)-BINAL-H as key steps. Addnl., preparation of bis-oxazole fragment I (R = H, R1 = CH2OSiPh2CMe3) was accomplished by the Barton-McCombie radical deoxygenation reaction of II.

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Pyrazine – Wikipedia,
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Electric Literature of C4H5N3. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about C-N Coupling of DNA-Conjugated (Hetero)aryl Bromides and Chlorides for DNA-Encoded Chemical Library Synthesis. Author is Chen, Ying-Chu; Faver, John C.; Ku, Angela F.; Miklossy, Gabriella; Riehle, Kevin; Bohren, Kurt M.; Ucisik, Melek N.; Matzuk, Martin M.; Yu, Zhifeng; Simmons, Nicholas.

DNA-encoded chem. library (DECL) screens are a rapid and economical tool to identify chem. starting points for drug discovery. As a robust transformation for drug discovery, palladium-catalyzed C-N coupling is a valuable synthetic method for the construction of DECL chem. matter; however, currently disclosed methods have only been demonstrated on DNA-attached (hetero)aromatic iodide and bromide electrophiles. We developed conditions utilizing an N-heterocyclic carbene-palladium catalyst that extends this reaction to the coupling of DNA-conjugated (hetero)aromatic chlorides with (hetero)aromatic and select aliphatic amine nucleophiles. In addition, we evaluated steric and electronic effects within this catalyst series, carried out a large substrate scope study on two representative (hetero)aryl bromides, and applied this newly developed method within the construction of a 63 million-membered DECL.

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