Category: 98-97-5

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

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

Category: Pyrazines. In 2020 NAT COMMUN published article about ASPARTATE DECARBOXYLASE; SUSCEPTIBILITY; PANTOTHENATE; MUTATIONS; MODEL in [Sun, Qingan; Li, Xiaojun; Sacchettini, James C.] Texas A&M Univ, Dept Biochem & Biophys, College Stn, TX 77843 USA; [Perez, Lisa M.] Texas A&M Univ, Lab Mol Simulat, College Stn, TX USA; [Shi, Wanliang; Zhang, Ying] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Dept Mol Microbiol & Immunol, Baltimore, MD 21205 USA in 2020, Cited 30. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis. It is active against the persistent, non-replicating mycobacteria responsible for the protracted therapy required to cure tuberculosis. Pyrazinamide is a pro-drug that is converted into pyrazinoic acid (POA) by pyrazinamidase, however, the exact target of the drug has been difficult to determine. Here we show the enzyme PanD binds POA in its active site in a manner consistent with competitive inhibition. The active site is not directly accessible to the inhibitor, suggesting the protein must undergo a conformational change to bind the inhibitor. This is consistent with the slow binding kinetics we determined for POA. Drug-resistant mutations cluster near loops that lay on top of the active site. These resistant mutants show reduced affinity and residence time of POA consistent with a model where resistance occurs by destabilizing the closed conformation of the active site. The important tuberculosis drug pyrazinamide (PZA) is converted to its active form pyrazinoic acid (POA) in Mycobacterium tuberculosis (Mtb). Here the authors identify the pantothenate biosynthesis pathway enzyme aspartate decarboxylase (PanD) as the target of PZA and determine the POA bound Mtb PanD crystal structure.

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

An article Revisiting problems and solutions to decrease Mycobacterium tuberculosis pyrazinamide false resistance when using the Bactec MGIT 960 system WOS:000466844000009 published article about SUSCEPTIBILITY in [Mustazzolu, Alessandro] Ist Super Sanita, Serv Comunicaz Sci, Rome, Italy; [Piersimoni, Claudio] AOU Osped Riuniti Ancona, Lab Patol Clin, Lab Unico Reg Diagnost Micobatteri, Ancona, Italy; [Iacobino, Angelo; Giannoni, Federico; Fattorini, Lanfranco] Ist Super Sanita, Dipartimento Malattie Infett, Viale Regina Elena 299, I-00161 Rome, Italy; [Chirullo, Barbara] Ist Super Sanita, Dipartimento Sicurezza Alimentare Nutr & Sanita P, Rome, Italy in 2019, Cited 22. SDS of cas: 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Pyrazinamide (PZA) is a first-line key drug used in combination with other agents for the treatment of tuberculosis (TB). Phenotypic and molecular assays for testing susceptibility of Mycobacterium tuberculosis (Mtb) to PZA have been developed, with the assay in liquid medium at acidic pH in the Bactec MGIT 960 (M960) system being routinely used in the mycobacteriology laboratories. However, false resistance to PZA by this method was reported to occur by several investigators, mostly due to high Mtb inoculum, which may impair drug activity by increasing the pH of the medium. In this study, a revision of the literature on the issue of false resistance in the M960 PZA assay was performed. In the reports examined, all improvements of the M960 test proposed to decrease false resistant results were based on the use of reduced inoculum densities of Mtb cells, to be easily translated into laboratory practice.

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

Formula: C5H4N2O2. In 2020 WASTE BIOMASS VALORI published article about TRANSFER HYDROGENATION; LEVULINIC ACID; ELECTROCATALYTIC HYDROGENATION; REDUCTIVE ETHERIFICATION; FURFURYL ALCOHOL; CONVERSION; TRANSFORMATION; HMF; 2,5-BIS(HYDROXYMETHYL)FURAN; DERIVATIVES in [Hu, Lei; Liu, Su; Song, Jie; Jiang, Yetao; He, Aiyong; Xu, Jiaxing] Huaiyin Normal Univ, Jiangsu Collaborat Innovat Ctr Reg Modern Agr & E, Sch Chem & Chem Engn, Jiangsu Key Lab Biomass Based Energy & Enzyme Tec, Huaian 223300, Peoples R China in 2020, Cited 82. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

By the simple assembly of zirconium tetrachloride and diethylenetriaminepentaacetic acid (DTPA), a new acid-base bifunctional zirconium-containing organic-inorganic nanohybrid catalyst (Zr-DTPA) was successfully prepared in this work, and then used for the catalytic transfer hydrogenation (CTH) of biomass-derived 5-hydroxymethylfurfural (HMF) into 2,5-dihydroxymethylfuran (DHMF) using isopropanol as the in situ hydrogen donor and reaction solvent. Satisfactorily, 98.7% HMF conversion and 95.2% DHMF yield could be achieved in 4 h at a moderate reaction temperature of 140 degrees C. After systematic studies, this excellent catalytic activity was proved to be mainly ascribed to the synergistic effect of Lewis-acidic sites (Zr4+) and Lewis-basic sites (O2- and N) with higher strengths and contents. Meanwhile, Zr-DTPA could be readily separated by filtration, when it was repeatedly used 5 recycles, its catalytic activity was not obviously changed, demonstrating that Zr-DTPA had good heterogeneity and reusability. More importantly, Zr-DTPA could also be employed to effectively catalyze the CTH of 5-methylfurfural, furfural, levulinic acid, ethyl levulinate and cyclohexanone into the corresponding products with high yields, indicating that it showed a superior universality for the selective hydrogenation of various biomass-derived carbonyl compounds.Graphical Abstract

Welcome to talk about 98-97-5, If you have any questions, you can contact Hu, L; Liu, S; Song, J; Jiang, YT; He, AY; Xu, JX or send Email.. Formula: C5H4N2O2

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

Authors Tomer, N; Goel, A; Ghule, VD; Malhotra, R in ELSEVIER published article about FLUORESCENT DETECTION; CHEMOSENSOR; PROBE; COPPER; PRECONCENTRATION; FE3+; SITE in [Tomer, Nisha; Goel, Apurva; Malhotra, Rajesh] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India; [Ghule, Vikas D.] Natl Inst Technol, Dept Chem, Kurukshetra 136119, Haryana, India in 2021, Cited 45. Quality Control of Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A new chromone based Schiff base ligand L was synthesized by the condensation of 3-formyl chromone and pyrazine-2-carbohydrazide as a colorimetric probe to detect Cu (II) ions selectively. An instant visual colour change from colourless to yellow was obtained on addition of Cu2+ ions to the probe L solution, while other metal ions found ineffective. The ligand L was characterized by H-1 NMR, FTIR and HRMS spectral techniques. UV-Visible spectroscopic technique was used to study the sensing ability of probe L for copper ions above other metal ions. The Job’s plot obtained from absorption studies and HRMS data confirmed that the Cu2+ ions bind with ligand L in 1:1 stoichiometric ratio. DFT computations were also supported the binding framework between L and Cu (II) ions. The LOD value and the association constant were obtained 3.9 x 10(-7) M and 2.3 x 10(5) M-1 respectively, via Benesi-Hildebrand equation. Selectivity of L towards Cu2+ ions was also studied and it was found that the probe L worked specifically for copper ions without any considerable influence of other intruding metal ions. In addition, in real water samples, the ligand L was fully implemented for identification and quantification of Cu2+ ions. (C) 2020 Elsevier B.V. All rights reserved.

Quality Control of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Tomer, N; Goel, A; Ghule, VD; Malhotra, R or send Email.

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

An article Mycobacterium tuberculosis PanD Structure-Function Analysis and Identification of a Potent Pyrazinoic Acid-Derived Enzyme Inhibitor WOS:000664331200009 published article about ASPARTATE-ALPHA-DECARBOXYLASE; PYRAZINAMIDE RESISTANCE; CRYSTAL-STRUCTURE; ATP SYNTHESIS; MUTATIONS; EXPRESSION; SYNTHASE in [Ragunathan, Priya; Latka, Chitra; Shin, Joon; Manimekalai, Malathy Sony Subramanian; Rishikesan, Sankaranarayanan; Gruber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore 637551, Singapore; [Cole, Malcolm; Hegde, Pooja; Aldrich, Courtney C.] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA; [Aragaw, Wassihun Wedajo; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Dick, Thomas] Hackensack Meridian Sch Med, Dept Med Sci, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20007 USA in 2021, Cited 28. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: Pyrazine-2-carboxylic acid

A common strategy employed in antibacterial drug discovery is the targeting of biosynthetic processes that are essential and specific for the pathogen. Specificity in particular avoids undesirable interactions with potential enzymatic counterparts in the human host, and it ensures ontarget toxicity. Synthesis of pantothenate (Vitamine B5), which is a precursor of the acyl carrier coenzyme A, is an example of such a pathway. In Mycobacterium tuberculosis (Mtb), which is the causative agent of tuberculosis (TB), pantothenate is formed by pantothenate synthase, utilizing D-pantoate and beta-Ala as substrates. beta-Ala is mainly formed by the decarboxylation of L-aspartate, generated by the decarboxylase PanD, which is a homo-oliogomer in solution. Pyrazinoic acid (POA), which is the bioactive form of the TB prodrug pyrazinamide, binds and inhibits PanD activity weakly. Here, we generated a library of recombinant Mtb PanD mutants based on structural information and PZA/POA resistance mutants. Alterations in oligomer formation, enzyme activity, and/or POA binding were observed in respective mutants, providing insights into essential amino acids for Mtb PanD’s proper structural assembly, decarboxylation activity and drug interaction. This information provided the platform for the design of novel POA analogues with modifications at position 3 of the pyrazine ring. Analogue 2, which incorporates a bulky naphthamido group at this position, displayed a 1000-fold increase in enzyme inhibition, compared to POA, along with moderately improved antimycobacterial activity. The data demonstrate that an improved understanding of mechanistic and enzymatic features of key metabolic enzymes can stimulate design of more-potent PanD inhibitors.

Recommanded Product: Pyrazine-2-carboxylic acid. 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

An article The molecular basis of pyrazinamide activity on Mycobacterium tuberculosis PanD WOS:000514636600005 published article about ASPARTATE DECARBOXYLASE; SUSCEPTIBILITY; PANTOTHENATE; MUTATIONS; MODEL in [Sun, Qingan; Li, Xiaojun; Sacchettini, James C.] Texas A&M Univ, Dept Biochem & Biophys, College Stn, TX 77843 USA; [Perez, Lisa M.] Texas A&M Univ, Lab Mol Simulat, College Stn, TX USA; [Shi, Wanliang; Zhang, Ying] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Dept Mol Microbiol & Immunol, Baltimore, MD 21205 USA in 2020, Cited 30. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Application In Synthesis of Pyrazine-2-carboxylic acid

Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis. It is active against the persistent, non-replicating mycobacteria responsible for the protracted therapy required to cure tuberculosis. Pyrazinamide is a pro-drug that is converted into pyrazinoic acid (POA) by pyrazinamidase, however, the exact target of the drug has been difficult to determine. Here we show the enzyme PanD binds POA in its active site in a manner consistent with competitive inhibition. The active site is not directly accessible to the inhibitor, suggesting the protein must undergo a conformational change to bind the inhibitor. This is consistent with the slow binding kinetics we determined for POA. Drug-resistant mutations cluster near loops that lay on top of the active site. These resistant mutants show reduced affinity and residence time of POA consistent with a model where resistance occurs by destabilizing the closed conformation of the active site. The important tuberculosis drug pyrazinamide (PZA) is converted to its active form pyrazinoic acid (POA) in Mycobacterium tuberculosis (Mtb). Here the authors identify the pantothenate biosynthesis pathway enzyme aspartate decarboxylase (PanD) as the target of PZA and determine the POA bound Mtb PanD crystal structure.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Sun, QG; Li, XJ; Perez, LM; Shi, WL; Zhang, Y; Sacchettini, JC or send Email.

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

In 2019 MOL NUTR FOOD RES published article about 5-HYDROXYPYRAZINOIC ACID; NICOTINIC-ACID; RAT; CONSUMPTION; MECHANISM; PLASMA; URINE in [Kremer, Jonathan I.; Pickard, Stephanie; Stadlmair, Lara F.; Glass-Theis, Anika; Buckel, Leon; Bakuradze, Tamara; Eisenbrand, Gerhard; Richling, Elke] Tech Univ Kaiserslautern, Dept Chem, Div Food Chem & Toxicol, Erwin Schrodinger Str 52, D-67663 Kaiserslautern, Germany in 2019, Cited 33. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Product Details of 98-97-5

Scope Coffee is a complex mixture of over 1000 compounds, including diverse heteroaromatic compounds such as alkylpyrazines. Little is known about the intake, metabolism, and bodily distribution of these compounds. Therefore, a human intervention study is conducted to investigate the excretion of alkylpyrazine metabolites in urine after the ingestion of brewed coffee containing alkylpyrazines. Methods and results After consuming a diet without heat-processed food, ten volunteers consumed 500 mL of freshly brewed coffee prepared from coffee pads, providing intakes of 2-methylpyrazine (2-MeP), 2,5-dimethylpyrazine (2,5-DMeP), and 2,6-dimethylpyrazine (2,6-DMeP) amounting to 17.2, 4.4, and 4.9 mu mol, respectively. These alkylpyrazines are metabolized into the corresponding pyrazine carboxylic acids, namely pyrazine-2-carboxylic acid (PA), 5-hydroxypyrazine-2-carboxylic acid (5-OHPA), 5-methylpyrazine-2-carboxylic acid (5-MePA), and 6-methylpyrazine-2-carboxylic acid (6-MePA). In total, 64% of the ingested 2-MeP is excreted as PA, as well as 26% as 5-OHPA, while 91% and 97% of the ingested 2,5-DMeP and 2,6-DMeP are recovered as 5-MePA and 6-MePA, respectively, in urine samples collected after coffee consumption. Conclusion This study provides evidence that alkylpyrazines are rapidly metabolized into the corresponding carboxylic acids and excreted via urine by humans, which is consistent with earlier rodent studies.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Kremer, JI; Pickard, S; Stadlmair, LF; Glass-Theis, A; Buckel, L; Bakuradze, T; Eisenbrand, G; Richling, E 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 PHARMACEUTICAL COCRYSTALS; SALTS; DESIGN; POLYMORPHISM; INVESTIGATE; SOLUBILITY; STABILITY; BEHAVIOR; COFORMER; LIQUID, Saw an article supported by the FAPESP foundation (Brazil)Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2013/09022-7, 2017/14936-9, 2018/12463-9, 2018/24378-6]; CNPq foundation (Brazil)Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPQ) [141829/2017-6]; CAPES foundation (Brazil)Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]; CPID/CDMF foundation (Brazil). Published in SPRINGER in DORDRECHT ,Authors: de Almeida, AC; Ferreira, PO; Torquetti, C; Ekawa, B; Carvalho, ACS; dos Santos, EC; Caires, F. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Novel cocrystals of ciprofloxacin with pyrazinoic acid and p-aminobenzoic acid in the 1:1 stoichiometric ratio were obtained by the mechanochemical method, under conditions of liquid-assisted grinding (LAG/ethanol) and neat grinding. They were characterized by powder X-ray diffractometry, infrared spectroscopy, simultaneous thermogravimetry, differential thermal analysis, differential scanning calorimetry (DSC) and DSC-Microscopy system. The results confirmed the successful synthesis of the cocrystals and indicated the functional groups responsible for the formation of the new supramolecular synthons. In addition, from the thermal analysis, it was possible to evaluate the thermal stability, composition, crystallization processes during heating, polymorphic transitions and construct the binary phase diagrams.

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