Category: 98-97-5

I found the field of Chemistry very interesting. Saw the article Stereodirecting Effect of C3-Ester Groups on the Glycosylation Stereochemistry of L-Rhamnopyranose Thioglycoside Donors: Stereoselective Synthesis of alpha- and beta-L-Rhamnopyranosides published in 2019. Computed Properties of C5H4N2O2, Reprint Addresses Yang, JS (corresponding author), Sichuan Univ, West China Hosp, Key Lab Drug Targeting & Drug Delivery Syst, Sichuan Engn Lab Plant Sourced Drug,Educ Minist, Chengdu 610041, Sichuan, Peoples R China.; Yang, JS (corresponding author), Sichuan Univ, West China Hosp, West China Sch Pharm, Sichuan Res Ctr Drug Precis Ind Technol, Chengdu 610041, Sichuan, Peoples R China.; Yang, JS (corresponding author), Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

The tuning effect of C3-ester groups on the glycosylation stereochemistry of L-rhamnopyranose (L-Rha) ethyl thioglycoside donors is described. On one hand, the L-Rha thioglycoside donors carrying 3-O-arylcarbonyl or levulinoyl group undergo highly alpha-selective glycosylation to afford a wide variety of alpha-L-rhamnoside products in high chemical yields. On the other hand, the glycosylation of the 3-O-4-nitropicoloyl and 2-pyrazinecarbonyl group substituted L-Rha thioglycosides displays beta-stereoselectivity. Only or predominant beta anomeric products are obtained when these L-Rha donors couple with the primary or reactive secondary acceptors, while the beta-selectivity may decrease significantly when these donors react with less reactive secondary alcohols. The synthetic utility of the newly developed alpha- and beta-directing L-Rha donors 1h and 1e has been demonstrated by the efficient synthesis of a structurally unique trisaccharide 9, which is derived from the cell wall polysaccharide of Sphaerotilus natans.

Welcome to talk about 98-97-5, If you have any questions, you can contact Lei, JC; Ruan, YX; Luo, S; Yang, JS or send Email.. Computed Properties of C5H4N2O2

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

An article Pyrazinamide triggers degradation of its target aspartate decarboxylase WOS:000564272800001 published article about TUBERCULOSIS; RESISTANCE; MUTATIONS; PROTEASE; COMPLEX in [Gopal, Pooja; Sarathy, Jickky Palmae] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Med, Singapore, Singapore; [Yee, Michelle; Dick, Thomas] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Microbiol & Immunol, Singapore, Singapore; [Ragunathan, Priya; Shin, Joon; Bhushan, Shashi; Grueber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore, Singapore; [Zhu, Junhao; Akopian, Tatos; Kandror, Olga; Rubin, Eric J.] Harvard Univ, Harvard TH Chan Sch Publ Hlth, Dept Immunol & Infect Dis, Boston, MA 02115 USA; [Lim, Teck Kwang; Lin, Qingsong] Natl Univ Singapore, Dept Biol Sci, Singapore, Singapore; [Gengenbacher, Martin; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Gengenbacher, Martin; Dick, Thomas] Seton Hall Univ, Dept Med Sci, Hackensack Meridian Med Sch, Nutley, NJ 07110 USA; [Gopal, Pooja] Merck Res Labs, MSD Translat Med Res Ctr, Singapore, Singapore in 2020, Cited 29. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: 98-97-5

Pyrazinamide is a sterilizing first-line tuberculosis drug. Genetic, metabolomic and biophysical analyses previously demonstrated that pyrazinoic acid, the bioactive form of the prodrug pyrazinamide (PZA), interrupts biosynthesis of coenzyme A in Mycobacterium tuberculosis by binding to aspartate decarboxylase PanD. While most drugs act by inhibiting protein function upon target binding, we find here that pyrazinoic acid is only a weak enzyme inhibitor. We show that binding of pyrazinoic acid to PanD triggers degradation of the protein by the caseinolytic protease ClpC1-ClpP. Thus, the old tuberculosis drug pyrazinamide exerts anti-bacterial activity by acting as a target degrader, a mechanism of action that has recently emerged as a successful strategy in drug discovery across disease indications. Our findings provide the basis for the rational discovery of next generation PZA.

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

An article Population Pharmacokinetic Modelling of Pyrazinamide and Pyrazinoic Acid in Patients with Multi-Drug Resistant Tuberculosis WOS:000475724600006 published article about RENAL-FUNCTION; METABOLITES; CLEARANCE; RIFAMPIN in [Mugabo, Pierre; Mulubwa, Mwila] Univ Western Cape, Sch Pharm, Private Bag X17, ZA-7535 Bellville, Cape Town, South Africa in 2019, Cited 28. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Safety of Pyrazine-2-carboxylic acid

Background and ObjectivesPyrazinamide, a drug used in the regimen for the treatment of drug-sensitive tuberculosis, is also used for the treatment of multidrug-resistant tuberculosis (MDR-TB). We aimed to describe the population pharmacokinetics of pyrazinamide and its major metabolite, pyrazinoic acid, in patients with MDR-TB and characterise the effects of demographic variables.MethodsThis was a non-randomised clinical study involving 51 adult patients admitted for the intensive phase of MDR-TB treatment. Blood samples were collected at pre-dose and at 0.5, 1, 1.5, 2, 3, 4, 8, 16 and 24h after drug administration. Plasma concentrations of pyrazinamide and pyrazinoic acid were analysed using a validated LC-MS/MS method. Nonlinear mixed-effects modelling using Monolix 2018R1 software was employed to estimate population pharmacokinetic parameters.ResultsA one-compartment pharmacokinetic model with transit compartment absorption process and first-order elimination best described the pyrazinamide and pyrazinoic acid concentration-time data. The estimated population pharmacokinetic parameters were 0.7h, 3.38h(-1), 57.1l, 4.37L/h and 10.5L/h for mean transit time, absorption rate constant, apparent distribution volume for pyrazinamide, and apparent clearance for pyrazinamide and pyrazinoic acid (CLm/F), respectively. These parameters were not affected by patient age, HIV status or sex. The parameter variability in CLm/F was the highest (83.5%), while the rest of the parameters ranged from 16.2 to 58%.ConclusionsThe developed population pharmacokinetic model adequately described the disposition of pyrazinamide and pyrazinoic acid and can be useful for dose determination of pyrazinamide in patients with MDR-TB.

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

Yao, H; Xie, SW; Ma, XQ; Liu, JK; Wu, HY; Lin, AJ; Yao, HQ; Li, DH; Xu, ST; Yang, DH; Chen, ZS; Xu, JY in [Yao, Hong; Xie, Shaowen; Ma, Xiaoqian; Liu, Junkai; Wu, Hongyu; Lin, Aijun; Yao, Hequan; Xu, Shengtao; Xu, Jinyi] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China; [Yao, Hong; Xie, Shaowen; Ma, Xiaoqian; Liu, Junkai; Wu, Hongyu; Lin, Aijun; Yao, Hequan; Xu, Shengtao; Xu, Jinyi] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China; [Li, Dahong] Shenyang Pharmaceut Univ, Sch Tradit Chinese Mat Med, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China; [Yang, Dong-Hua; Chen, Zhe-Sheng] St Johns Univ, Coll Pharm & Hlth Sci, Queens, NY 11439 USA published Identification of a Potent Oridonin Analogue for Treatment of Triple-Negative Breast Cancer in 2020, Cited 46. Category: Pyrazines. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Triple-negative breast cancer (TNBC) is one of the most highly invasive and metastatic breast cancers without safe and effective therapeutic drugs. The natural product oridonin is reported to be a potential anti-TNBC agent. However, its moderate activity and complex structure hampered its clinical application. In this study, the novel oridonin analogues were first identified by removal of multiple hydroxyl groups and structural simplification of oridonin. The representative analogue 20 exhibited potent anticancer effects. Further structural modification on 20 generated the most potent derivative 56, which possessed 120-fold more potent antiproliferative activity than oridonin in the TNBC cell line HCC1806. Importantly, compound 56 exhibited more potent anticancer activity than paclitaxel in TNBC xenograft nude mice. Moreover, 56 could attenuate the expression of MMP-2, MMP-9, p-FAK, and integrin beta 1 to inhibit TNBC cell metastasis. All results suggest that compound 56 may warrant further investigation as a promising candidate agent for the treatment of TNBC.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Yao, H; Xie, SW; Ma, XQ; Liu, JK; Wu, HY; Lin, AJ; Yao, HQ; Li, DH; Xu, ST; Yang, DH; Chen, ZS; Xu, JY or send Email.

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

Name: Pyrazine-2-carboxylic acid. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of novel TNNI3K inhibitor suppresses pyroptosis and apoptosis in murine myocardial infarction injury published in 2020, Reprint Addresses He, G (corresponding author), Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China.; He, G (corresponding author), Sichuan Univ, West China Hosp, Canc Ctr, Chengdu 610041, Sichuan, Peoples R China.; He, G (corresponding author), Collaborat Innovat Ctr, Chengdu 610041, Sichuan, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

Myocardial infarction (MI) injury is a highly lethal syndrome that has, until recently, suffered from a lack of clinically efficient targeted therapeutics. The cardiac troponin I interacting kinase (TNNI3K) exacerbates ischemia-reperfusion (IR) injury via oxidative stress, thereby promoting cardiomyocyte death. In this current study, we designed and synthesized 35 novel TNNI3K inhibitors with a pyrido[4,5]thieno [2,3-d] pyrimidine scaffold. In vitro results indicated that some of the inhibitors exhibited sub-micromolar TNNI3K inhibitory capacity and good kinase selectivity, as well as cytoprotective activity, in an oxygen-glucose deprivation (OGD) injury cardiomyocyte model. Furthermore, investigation of the mechanism of the representative derivative compound 6o suggested it suppresses pyroptosis and apoptosis in cardiomyocytes by interfering with p38MAPK activation, which was further confirmed in a murine myocardial infarction injury model. In vivo results indicate that compound 6o can markedly reduce myocardial infarction size and alleviate cardiac tissue damage in rats. In brief, our results provide the basis for further development of novel TNNI3K inhibitors for targeted MI therapy. (C) 2020 Elsevier Masson SAS. All rights reserved.

Name: 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

COA of Formula: C5H4N2O2. Zhao, FY; Sun, X; Lu, W; Xu, L; Shi, JZ; Yang, SL; Zhou, MY; Su, F; Lin, F; Cao, FL in [Zhao, Fengyi; Xu, Li; Cao, Fuliang] Nanjing Forestry Univ, Coinnovat Ctr Sustainable Forestry Southern China, Nanjing 210037, Peoples R China; [Zhao, Fengyi; Cao, Fuliang] Nanjing Forestry Univ, Coll Forestry, Nanjing, Peoples R China; [Zhao, Fengyi; Sun, Xu; Lu, Wen; Xu, Li; Shi, Jiuzhou] Nanjing Forestry Univ, Coll Sci, Nanjing, Peoples R China; [Sun, Xu] Nanjing Forestry Univ, Coll Informat Sci & Technol, Nanjing, Peoples R China; [Yang, Shilong; Zhou, Mengyi; Su, Fan; Lin, Feng] Nanjing Forestry Univ, Adv Anal & Testing Ctr, Nanjing, Peoples R China published Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives as potential antiproliferative and apoptosis-inducing agents in 2020, Cited 60. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Several dehydroabietylamine derivatives containing heterocyclic moieties such as thiophene and pyrazine ring were successfully synthesized. The antiproliferative activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides were investigated in vitro against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver), and HUVEC (umbilical vein) cells by MTT assay. The toxicity of L-1-L-10 (IC50 = 5.92- >100 mu M) was lower than L-0 (1.27 mu M) and DOX (4.40 mu M) in every case. Compound L-1 had higher anti-HepG2 (0.66 mu M), anti-MCF-7 (5.33 mu M), and anti-A549 (2.11 mu M) and compound L-3 had higher anti-HepG2 (1.63 mu M) and anti-MCF-7 (2.65 mu M) activities. Both of these compounds were recognized with high efficiency in apoptosis induction in HepG2 cells and intercalated binding modes with DNA. Moreover, with average IC50 values of 0.66 and 5.98 mu M, L-1 was nine times more effective at suppressing cultured HepG2 cells viability than normal cells (SI = 9). The relative tumor proliferation rate (T/C) was 38.6%, the tumor inhibition rate was up to 61.2%, which indicated that L-1 had no significant toxicity but high anti-HepG2 activity in vivo. Thus, it may be a potential antiproliferation drug with nontoxic side effects.

Welcome to talk about 98-97-5, If you have any questions, you can contact Zhao, FY; Sun, X; Lu, W; Xu, L; Shi, JZ; Yang, SL; Zhou, MY; Su, F; Lin, F; Cao, FL or send Email.. COA of Formula: C5H4N2O2

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

Recently I am researching about ONE-POT SYNTHESIS; 2-SUBSTITUTED BENZOTHIAZOLES; OXIDATIVE CYCLIZATION; CATALYST; EFFICIENT; 2-ARYLBENZOXAZOLES; BASES, Saw an article supported by the . Published in WILEY in HOBOKEN ,Authors: Kashid, BB; Ghanwat, AA; Khedkar, VM; Dongare, BB; Shaikh, MH; Deshpande, PP; Wakchaure, YB. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. Recommanded Product: 98-97-5

A series of novel 2-substituted benzimidazole and benzoxazole derivatives as a potential antimicrobial and antioxidant agent were synthesized via coupling of N-methyl-o-phenylenediamine or 2-amino-phenol with aromatic aldehyde and acid in the presence of polyphosphoric acid as an efficient catalyst as well as solvent by conventional method in short reaction times with excellent yield. The newly synthesized benzimidazole and benzoxazole derivatives were evaluated for antimicrobial and antioxidant activity and exhibited excellent to good activities compared to the standard drugs. Furthermore, the theoretical predictions based on molecular docking against microbial DNA gyrase could provide an insight into the plausible mechanism of action and establish a link between the observed antimicrobial activity and the binding affinity shedding light on specific thermodynamic (bonded and nonbonded) interactions governing the activity. Furthermore, the synthesized compounds were analyzed for absorption, distribution, metabolism, and excretion properties and exhibited potential properties to build up as good oral drug candidates.

Welcome to talk about 98-97-5, If you have any questions, you can contact Kashid, BB; Ghanwat, AA; Khedkar, VM; Dongare, BB; Shaikh, MH; Deshpande, PP; Wakchaure, YB or send Email.. Recommanded Product: 98-97-5

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

Category: Pyrazines. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Influence of the introduction of a triphenylphosphine group on the anticancer activity of a copper complex published in 2020, Reprint Addresses Zhao, JA; Hu, JY (corresponding author), Henan Univ Urban Construct, Coll Mat & Chem Engn, Pingdingshan 467036, Henan, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

Aiming at obtaining new copper complexes with good cytotoxicity against cancer cells, triphenylphosphine (TPP) was introduced to obtain insight into the influence of the co-ligands. In this paper, two copper complexes, Cu(2-pbmq)(CH3OH)Br-2 (1) and [Cu(2-pbmq)(TPP)Br](2) (2) were designed, synthesized, and characterized by X-ray crystallography, 2-((2-(pyrazin-2-yl)-1H-benzo[d]imidazol-1-yl)methyl))quinolone (2-pbmq), to investigate the influence of the TPP group on the anticancer activity of the metal complex. Although the presence of the TPP group diminished the intensity of the interaction properties of the complex with DNA, the in vitro anticancer activity and cellular uptake of the TPP-containing complex were markedly superior to those of its TPP-lacking counterpart. Detailed studies on the more potently cytotoxic complex 2 revealed that it accumulated in nucleus, arrested the cell cycle at the G0-G1 phase, causing mitochondrial dysfunction, involving the potential simultaneous mitochondrial membrane collapse, cellular ATP level depletion, and Ca2+ leakage, eventually inducing cell apoptosis. In summary, the introduction of a TPP group enhances the biological activity and cytotoxicity of the complex.

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.. Category: Pyrazines

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

Recommanded Product: Pyrazine-2-carboxylic acid. Authors Dumpala, RMR; Das, SK; Ali, M; Boda, A; Kumar, P; Rawat, N; Kumar, A; Ali, SM in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Dumpala, Rama Mohana Rao; Rawat, Neetika] Bhabha Atom Res Ctr, Radiochem Div, Mumbai 400094, Maharashtra, India; [Das, Sourav Kumar; Ali, Manjoor; Kumar, Amit] Bhabha Atom Res Ctr, Radiat Biol & Hlth Sci Div, Mumbai 400094, Maharashtra, India; [Boda, Anil; Ali, Sk Musharaf] Bhabha Atom Res Ctr, Chem Engn Div, Mumbai 400094, Maharashtra, India; [Kumar, Pranaw] Bhabha Atom Res Ctr, Fuel Chem Div, Mumbai 400094, Maharashtra, India in 2021, Cited 78. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Thorium (Th) exposure to the human beings is a radiochemical hazard and the chelation therapy by suitable drugs is the major prevention approach to deal with. The present studies aimed at usage of pyrazinoic acid (PCA), which is a prodrug to treat tuberculosis, for its usage as decorporating agent for thorium from human body. The present studies provide a comprehensive knowledge on the chemical interaction and biological efficacy of pyrazinoic acid (PCA) for decorporation of Thorium from the human body. The thermodynamic parameters for Th-PCA speciation are determined by both experiment and theory. The potentiometric data analysis and Electro-Spray Ionization Mass Spectrometry (ESI-MS) studies revealed the formation of MLi (i = 1-4) species with the decrease in stepwise stability constants. All the species formations are endothermic reactions and are predominantly entropy-driven. Biological experiments using human erythrocytes, whole blood and normal human lung cells showed cytocompatibility and decorporation ability of PCA for Thorium. Density functional calculations have been carried out to get insights on interaction process at molecular level. The experimental results and theoretical predictions found to be in line with each other. Present findings on complexation of Th by PCA and its evaluation in human cells and blood would further motivate determination of its safety levels and decorporation efficacy in animal models. (C) 2021 Elsevier Ltd. All rights reserved.

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

Safety of Pyrazine-2-carboxylic acid. In 2019 J CLIN MICROBIOL published article about PNCA MUTATIONS; PYRAZINOIC ACID; MGIT 960; PREVALENCE; EFFLUX; TESTS in [Alcantara, Roberto; Fuentes, Patricia; Antiparra, Ricardo; Santos, Marco; Zimic, Mirko; Sheen, Patricia] Univ Peruana Cayetano Heredia, Lab Bioinformat & Biol Mol, Fac Ciencias & Filosofia, Lima, Peru; [Gilman, Robert H.] Johns Hopkins Bloomberg Sch Publ Hlth, Dept Int Hlth, Baltimore, MD USA; [Kirwan, Daniela E.] St Georges Univ London, Inst Infect & Immun, London, England in 2019, Cited 45. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Although pyrazinamide (PZA) is a key component of first- and second-line tuberculosis treatment regimens, there is no gold standard to determine PZA resistance. Approximately 50% of multidrug-resistant tuberculosis (MDR-TB) and over 90% of extensively drug-resistant tuberculosis (XDR-TB) strains are also PZA resistant. pncA sequencing is the endorsed test to evaluate PZA susceptibility. However, molecular methods have limitations for their wide application. In this study, we standardized and evaluated a new method, MODS-Wayne, to determine PZA resistance. MODS-Wayne is based on the detection of pyrazinoic acid, the hydrolysis product of PZA, directly in the supernatant of sputum cultures by detecting a color change following the addition of 10% ferrous ammonium sulfate. Using a PZA concentration of 800 mu g/ml, sensitivity and specificity were evaluated at three different periods of incubation (reading 1, reading 2, and reading 3) using a composite reference standard (MGIT-PZA, pncA sequencing, and the classic Wayne test). MODS-Wayne was able to detect PZA resistance, with a sensitivity and specificity of 92.7% and 99.3%, respectively, at reading 3. MODS-Wayne had an agreement of 93.8% and a kappa index of 0.79 compared to the classic Wayne test, an agreement of 95.3% and kappa index of 0.86 compared to MGIT-PZA, and an agreement of 96.9% and kappa index of 0.90 compared to pncA sequencing. In conclusion, MODS-Wayne is a simple, fast, accurate, and inexpensive approach to detect PZA resistance, making this an attractive assay especially for low-resource countries, where TB is a major public health problem.

Welcome to talk about 98-97-5, If you have any questions, you can contact Alcantara, R; Fuentes, P; Antiparra, R; Santos, M; Gilman, RH; Kirwan, DE; Zimic, M; Sheen, P or send Email.. Safety of Pyrazine-2-carboxylic acid

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