Month: November 2021

An article Reduction in Coordination Number of Eu(III) on Complexation with Pyrazine Mono- and Di-Carboxylates in Aqueous Medium WOS:000482173300084 published article about MONOCARBOXYLATE-N-OXIDES; LIQUID-LIQUID-EXTRACTION; 2-PYRAZINECARBOXYLIC ACID; THEORETICAL INSIGHTS; LUMINESCENCE; SEPARATION; EUROPIUM(III); EU3+; LANTHANIDES; SELECTIVITY in [Dumpala, Rama Mohana Rao; Rawat, Neetika] Bhabha Atom Res Ctr, Radioanalyt Chem Div, Mumbai 400085, Maharashtra, India; [Boda, Anil; Ali, Sk. Musharaf] Bhabha Atom Res Ctr, Chem Engn Div, Mumbai 400085, Maharashtra, India; [Kumar, Pranaw] Bhabha Atom Res Ctr, Fuel Chem Div, Mumbai 400085, Maharashtra, India in 2019, Cited 52. Recommanded Product: 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The denticity, flexibility, and steric hindrance of the ligand are key factors in deciding the mode and number of coordination around a metal ion on complex formation. The thermodynamic aspects of lanthanide complexation with various multidentate ligands provides a significant insight into understand the coordination chemistry of lanthanides in framing the relevant metal organic networks for the applications in biological, biochemical and medical aspects. The pyrazine carboxylic acids are known to form many structurally important complexes and further can form chelates with coordination number of eight for europium in which more water molecules can be knocked out from the primary coordination sphere than demanded by denticity of the ligand. The present studies aimed at ESI-MS characterization and determination of the thermodynamic parameters (log beta, Delta G, Delta H, and Delta S), luminescence properties of europium complexes with pyrazine-2-carboxylate and pyrazine-2,3-dicarboxylate in aqueous solutions by experiment as well as theory. Time resolved luminescence spectroscopy supported by DFT calculations are carried out to optimize the stable geometries of the complexes with various modes of binding and coordination. Furthermore, the thermodynamic parameters estimated theoretically have been used to trace the path of complex formation.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Computed Properties of C5H4N2O2. Authors Yang, YJ; Wang, K; Yang, Y; Lai, FF; Chen, XG; Xiao, ZY in TAYLOR & FRANCIS LTD published article about in [Yang, Ya-Jun; Wang, Ke; Yang, Ying; Xiao, Zhi-Yan] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Active Subst Discovery & Druggabi, Beijing 100050, Peoples R China; [Lai, Fang-Fang; Chen, Xiao-Guang] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China in 2021, Cited 21. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Based on the interaction modes of the natural 20S proteasome inhibitors TMC-95A, we have previously discovered a dipeptide 1. To explore the SAR around compound 1, we designed and synthesized a series of dipeptides (8-38) with a fragment-based strategy. Among them, nine compounds showed significant inhibitory activities against the chymotrypsin-like activity of human 20S proteasome with IC50 values at the submicromolar level, which were comparable or even superior to the parent compound 1. Meanwhile, they displayed no significant inhibition against trypsin-like and caspase-like activities of 20S proteasome. The results suggested the feasibility to design dipeptides as novel and potent 20S proteasome inhibitors.

Computed Properties of C5H4N2O2. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of Pyrazine-2-carboxylic acid. In 2020 J MED CHEM published article about BENZOXAZINYL-OXAZOLIDINONES; MYCOBACTERIUM-TUBERCULOSIS; BACTERICIDAL ACTIVITY; IN-VITRO; POTENT; ANALOGS; DESIGN in [Zhao, Hongyi; Li, Gang; Lu, Haijia; Huang, Haihong; Zhang, Dongfeng] Chinese Acad Med Sci & Peking Union Med Coll, Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Key Lab AntiDR TB Innovat Drug Res,Inst Mat Med, Beijing 100050, Peoples R China; [Wang, Bin; Fu, Lei; Lu, Yu] Capital Med Univ, Beijing Chest Hosp, Beijing TB & Thorac Tumor Res Inst, Beijing Key Lab Drug Resistance TB Res,Dept Pharm, Beijing 101149, Peoples R China; [Liu, Yuke; Sheng, Li; Li, Yan] Chinese Acad Med Sci & Peking Union Med Coll, Chinese Acad Med Sci, Beijing Key Lab Nonclin Drug Metab & PK PD Study, Key Lab AntiDR TB Innovat Drug Res,Inst Mat Med, Beijing 100050, Peoples R China; [Zhang, Baoxi; Lu, Yang] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China; [Ma, Chen] Chinese Acad Med Sci & Peking Union Med Coll, Chinese Acad Med Sci, Beijing Key Lab Polymorph Drugs, Key Lab AntiDR TB Innovat Drug Res,Inst Mat Med, Beijing 100050, Peoples R China in 2020, Cited 30. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Tuberculosis (TB) remains a serious public health challenge, and the research and development of new anti-TB drugs is an essential component of the global strategy to eradicate TB. In this work, we discovered a conformationally constrained oxazolidinone 19c with improved anti-TB activity and safety profile through a focused lead optimization effort. Compound 19c displayed superior in vivo efficacy in a mouse TB infection model compared to linezolid and sutezolid. The druggability of compound 19c was demonstrated in a panel of assays including microsomal stability, cytotoxicity, cytochrome P450 enzyme inhibition, and pharmacokinetics in animals. Compound 19c demonstrated an excellent safety profile in a battery of safety assays, including mitochondrial protein synthesis, hERG K+, hCav1.2, and Nav1.5 channels, monoamine oxidase, and genotoxicity. In a 4 week repeated dose toxicology study in rats, 19c appeared to have less bone marrow suppression than linezolid, which has been a major liability of the oxazolidinone class.

Welcome to talk about 98-97-5, If you have any questions, you can contact Zhao, HY; Wang, B; Fu, L; Li, G; Lu, HJ; Liu, YK; Sheng, L; Li, Y; Zhang, BX; Lu, Y; Ma, C; Huang, HH; Zhang, DF; Lu, Y or send Email.. Quality Control of Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

COA of Formula: C5H4N2O2. Authors Alsayed, SSR; Lun, SC; Payne, A; Bishai, WR; Gunosewoyo, H in WILEY published article about in [Alsayed, Shahinda S. R.; Gunosewoyo, Hendra] Curtin Univ, Fac Hlth Sci, Sch Pharm & Biomed Sci, Perth, WA, Australia; [Lun, Shichun; Bishai, William R.] Johns Hopkins Sch Med, Dept Med, Ctr TB Res, Div Infect Dis, Baltimore, MD 21205 USA; [Payne, Alan] Curtin Univ, Sch Mol & Life Sci, Perth, WA, Australia; [Bishai, William R.] Howard Hughes Med Inst, Chevy Chase, MD USA in 2021, Cited 54. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Several rationally designed isoniazid (INH), pyrazinamide (PZA) and ciprofloxacin (CPF) derivatives were conveniently synthesized and evaluated in vitro against H37Rv Mycobacterium tuberculosis (M. tb) strain. CPF derivative 16 displayed a modest activity (MIC = 16 mu g/ml) and was docked into the M. tb DNA gyrase. Isoniazid-pyrazinoic acid (INH-POA) hybrid 21a showed the highest potency in our study (MIC = 2 mu g/ml). It also retained its high activity against the other tested M. tb drug-sensitive strain (DS) V4207 (MIC = 4 mu g/ml) and demonstrated negligible cytotoxicity against Vero cells (IC50 >= 64 mu g/ml). Four tested drug-resistant (DR) M. tb strains were refractory to 21a, similar to INH, whilst being sensitive to CPF. Compound 21a was also inactive against two non-tuberculous mycobacterial (NTM) strains, suggesting its selective activity against M. tb. The noteworthy activity of 21a against DS strains and its low cytotoxicity highlights its potential to treat DS M. tb.

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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Name: Pyrazine-2-carboxylic acid. Khan, MT; Chinnasamy, S; Cui, ZL; Irfan, M; Wei, DQ in [Khan, Muhammad Tahir] Capital Univ Sci & Technol, Dept Bioinformat & Biosci, Islamabad, Pakistan; [Chinnasamy, Sathishkumar; Wei, Dong-Qing] Shanghai Jiao Tong Univ, State Key Lab Microbial Metab, Sch Life Sci & Biotechnol, Minist Educ, Shanghai 200240, Peoples R China; [Chinnasamy, Sathishkumar; Wei, Dong-Qing] Shanghai Jiao Tong Univ, Joint Lab Int Cooperat Metab & Dev Sci, Minist Educ, Shanghai 200240, Peoples R China; [Wei, Dong-Qing] Peng Cheng Lab, Vanke Cloud City Phase 1 Bldg 8,Xili St, Shenzhen 518055, Guangdong, Peoples R China; [Cui, Zhilei] Shanghai Jiao Tong Univ, Dept Resp Med, XinHua Hosp, Sch Med, Shanghai, Peoples R China; [Irfan, Muhammad] Univ Florida, Dept Microbiol & Cell Sci, Genet Inst, Gainesville, FL 32611 USA; [Irfan, Muhammad] Univ Florida, Inst Food & Agr Sci, Gainesville, FL 32611 USA published Mechanistic analysis of A46V, H57Y, and D129N in pyrazinamidase associated with pyrazinamide resistance in 2020, Cited 58. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyrazinamide (PZA) is a component of first-line drugs, active against latent Mycobacterium tuberculosis (MTB) isolates. The prodrug is activated into the active form, pyrazinoic acid (POA) via pncA gene-encoded pyrazinamidase (PZase). Mutations in pncA have been reported, most commonly responsible for PZA-resistance in more than 70% of the resistant cases. In our previous study, we detected many mutations in PZase among PZA-resistance MTB isolates including A46V, H71Y, and D129N. The current study was aimed to investigate the molecular mechanism of PZA-resistance behind mutants (MTs) A46V, H71Y, and D129N in comparison with the wild type (WT) through molecular dynamic (MD) simulation. MTB positive samples were subjected to PZA drug susceptibility testing (DST) against critical concentration (100ug/ml). The resistant samples were subjected to pncA sequencing. Thirty-six various mutations have been observed in the coding region of pncA of PZA-resistant isolates (GenBank accession No. MH461111) including A46V, H71Y, and D129N. The post-simulation analysis revealed a significant variation in MTs structural dynamics as compared to the WT. Root means square deviations (RMSD) and Root means square fluctuation (RMSF) has been found in variation between WT and MTs. Folding effect and pocket volume were altered in MTs when compared with WT. Geometric matching supports the effect of mutation A46V, H71Y, and D129N on PZase structure that may have an insight effect on PZase dynamics, making them vulnerable to convert pro-PZA into active form, POA. In conclusion, the current analyses will provide useful information behind PZA-resistance for better management of drug-resistant TB. (C) 2020 The Author(s). Published by Elsevier B.V. on behalf of King Saud University.

Welcome to talk about 98-97-5, If you have any questions, you can contact Khan, MT; Chinnasamy, S; Cui, ZL; Irfan, M; Wei, DQ or send Email.. Name: Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Synthesis, antimicrobial and chitinase inhibitory activities of 3-amidocoumarins published in 2020. SDS of cas: 98-97-5, Reprint Addresses Katiyar, D (corresponding author), Banaras Hindu Univ, Dept Chem, MMV, Varanasi 221005, Uttar Pradesh, India.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

A series of 3-amidocoumarins has been synthesized and tested in vitro for their anitimicrobial and chitinase inhibitory activities. Among these, compounds 5k, 5l, 8b-8d, 8f and 8g exhibited good antibacterial activity with MIC values in the range of 6.25-25 mu g/mL against some of the tested strains while compounds 5l, 8b, 8c and 8f showed good activity against at least one or two fungal strains. Some of the assayed compounds 5d, 5k, 5l, 8b and 8c displayed significant chitinase inhibitory activity with IC50, values in the range of 3.74-5.6 mu M. Among them, 5l proved to be potent chitinase inhibitor with IC50 value of 3.74 mu M. To better understand the enzyme-inhibitor interactions molecular docking study of all the synthesized compounds was carried out on Aspergillus fumigatus chitinase 1W9U. The compound 5l showed high binding affinity with the receptor with binding energy value of -8.44 Kcal/mol. This study also provides structure activity relationship (SAR) of synthesized compounds.

Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.. SDS of cas: 98-97-5

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In 2019 EUR J MED CHEM published article about MECHANISMS; IDENTIFICATION; INFLAMMASOME; CHEMOTAXIS in [Zhang, Zhenguo; Lu, Ran; Jiang, Cheng] China Pharmaceut Univ, Jiang Su Key Lab Drug Design & Optimizat, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Zhang, Zhenguo; Lu, Ran; Li, Baiyang; Meng, Zibo; Jiang, Cheng] China Pharmaceut Univ, Dept Med Chem, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Hao, Kun] China Pharmaceut Univ, State Key Lab Nat Med, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China; [Li, Hanwen; Liu, Chunxiao; Zhou, Mengze; Hu, Qinghua] China Pharmaceut Univ, Key Lab Drug Metab & Pharmacokinet, Tongjiaxiang 24, Nanjing 210009, Jiangsu, Peoples R China in 2019, Cited 35. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

The P2Y(14) receptor (P2Y(14)R) plays a key role in the modulation of inflammatory process, but very few classes of antagonists have been reported. A series of 3-amide benzoic acid derivatives were identified as novel and potent P2Y(14)R antagonists. The most potent antagonist, 16c, showed comparable activity (IC50 = 1.77 nM) to PPTN, the most potent P2Y(14)R antagonist reported. Compound 16c demonstrated dramatically improved aqueous solubility and excellent metabolic stability in rat and human microsomes. Investigation of the anti-inflammatory effect of 16c was performed in MSU treated THP-1 cells by flow cytometry, Western Blot and immunofluorescence labeling technology, which exhibited that 16c might be a promising candidate for further research. (C) 2019 Elsevier Masson SAS. All rights reserved.

Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Zhang, ZG; Hao, K; Li, HW; Lu, R; Liu, CX; Zhou, MZ; Li, BY; Meng, ZB; Hu, QH; Jiang, C or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: Pyrazine-2-carboxylic acid. Recently I am researching about BASIC SIDE-CHAINS; C-H CARBONYLATION; OXIDATIVE CARBONYLATION; DESIGN; C(SP(2))-H; INHIBITORS; BONDS; OPTIMIZATION; CYCLIZATION; ACTIVATION, Saw an article supported by the Zhejiang Natural Science Fund for Young Scholars [LQ18B020008]; Zhejiang Sci-Tech UniversityZhejiang University of Science & Technology [17062078-Y]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21772177]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Ying, J; Fu, LY; Zhong, GQ; Wu, XF. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

A cobalt-catalyzed C-H carbonylation of naphthylamides for the synthesis of benzo[cd]indol-2(1H)-one scaffolds has been developed. The reaction employs a traceless directing group and uses benzene-1,3,5-triyltriormate as the CO source, affording various free (NH)-benzo[cd]indol-2(1H)-ones in moderate to high yields (up to 88%). Using this protocol, the total synthesis of BET bromodomain inhibitors A and B was accomplished as well.

Recommanded Product: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Ying, J; Fu, LY; Zhong, GQ; Wu, XF or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recently I am researching about SUSCEPTIBILITY; IMMUNOASSAY, Saw an article supported by the Wellcome TrustWellcome TrustEuropean Commission [099805/Z/112/Z]. HPLC of Formula: C5H4N2O2. Published in PUBLIC LIBRARY SCIENCE in SAN FRANCISCO ,Authors: Florentini, EA; Angulo, N; Gilman, RH; Alcantara, R; Roncal, E; Antiparra, R; Toscano, E; Vallejos, K; Kirwan, D; Zimic, M; Sheen, P. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Pyrazinamide (PZA) susceptibility testing in Mycobacterium tuberculosis (Mtb) is a current area of development and PZA-resistant strains are increasingly prevalent. Previous studies have demonstrated that the detection of pyrazinoic acid (POA), the metabolite produced by the deamidation of PZA, is a good predictor for PZA resistance since a resistant strain would not convert PZA into POA at a critical required rate, whereas a susceptible strain will do, expelling POA to the extracellular environment at a certain rate, and allowing for quantification of this accumulated analyte. In order to quantify POA, an indirect competitive ELISA (icELISA) test using hyperimmune polyclonal rabbit serum against POA was developed: for this purpose, pure POA was first covalently linked to the highly immunogenic Keyhole Limpet Hemocyanine, and inoculated in rabbits. A construct made of bovine serum albumin (BSA) linked to pure POA and fixed at the bottom of wells was used as a competitor against spiked samples and liquid Mtb culture supernatants. When spiked samples (commercial POA alone) were analyzed, the half maximal inhibitory concentration (IC50) was 1.16 mg/mL, the limit of detection 200 mu g/mL and the assay was specific (it did not detect PZA, IC50 > 20 mg/mL). However, culture supernatants (7H9-OADC-PANTA medium) disrupted the competition and a proper icELISA curve was not obtainable. We consider that, although we have shown that it is feasible to induce antibodies against POA, matrix effects could damage its analytical usefulness; multiple, upcoming ways to solve this obstacle are suggested.

HPLC of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Florentini, EA; Angulo, N; Gilman, RH; Alcantara, R; Roncal, E; Antiparra, R; Toscano, E; Vallejos, K; Kirwan, D; Zimic, M; Sheen, P or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In 2019 DALTON T published article about AQUEOUS-SOLUTION; EQUILIBRIUM-CONSTANTS; CARBOXYLIC-ACIDS; URANIUM(VI); CRYSTAL; ION; CHEMISTRY; LIGAND in [Lv, Lina; Chen, Baihua; Liu, Jun; Yang, Yanqiu] China Acad Engn Phys, Inst Nucl Phys & Chem, Mianyang 621900, Sichuan, Peoples R China; [Chen, Jing; Xu, Chao] Tsinghua Univ, Inst Nucl & New Energy Technol, Beijing 100084, Peoples R China in 2019, Cited 42. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. SDS of cas: 98-97-5

Complexation of U(vi) with pyridazine-3-carboxylate (PDZ) and pyrazine-2-carboxylate (PAZ) was studied by spectrophotometry, potentiometry and microcalorimetry in 1.0 mol dm(-3) NaClO4. Three complexes, [UO2L](+), UO2L2(aq) and [UO2L3](-), were identified and their stability constants (log) and the corresponding formation enthalpies were determined. The thermodynamic parameters indicate that the formation of the three complexes is endothermic and driven exclusively by entropy. H-1 and C-13-NMR data provide insight into the coordination modes of the complexes which corroborate with the thermodynamic data. Ligands chelate to U(vi) via (2)(N,O) coordination mode in complexes [UO2L](+) and UO2L2(aq). The crystal structures of four U(vi) complexes, [(UO2)(PAZ)(2)(H2O)]H2O(i), [(UO2)(PDZ)(2)(H2O)](ii), [(UO2)(PDZ)(3)Na2ClO4]2H(2)O(iii), and [(UO2)(2)(PDZ)(4)(H2O)(2)]2H(2)O(iv), were determined by single-crystal X-ray diffraction and compared with the U(vi) complex with picolinate (PA) (CH6N3)[UO2(PA)(3)] in the literature. The structure data suggest that the carboxylates coordinate with uranium in O?C-O-U mode. The strengths of the U-O-C-C-N chelate cycles in the U(vi)/L complexes decrease with the trend of PA > PDZ > PAZ, which is in great agreement with the trend of thermodynamic parameters in aqueous solutions. It is interesting that in compound II two PDZ molecules coordinate with U(vi) in cis-planar positions via (2)(N,O) mode, but in other metal complexes of the three ligands having the same (2)(N,O) coordination mode the two ligand molecules are all in trans-arrangement. In the dimeric complex IV, one ligand coordinate with U(vi) in (2)(N,O) mode, while the other does it in (2)-L-(2)(O:O) mode respectively.

SDS of cas: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Lv, LN; Chen, BH; Liu, J; Chen, J; Xu, C; Yang, YQ or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem