Pyrazines

An article Pyrazinamide resistance and mutations in pncA among isolates of Mycobacterium tuberculosis from Khyber Pakhtunkhwa, Pakistan WOS:000458381700012 published article about DRUG-RESISTANCE; GENE; SUSCEPTIBILITY; PREVALENCE; RPSA in [Khan, Muhammad Tahir; Malik, Shaukat Iqbal] Capital Univ Sci & Technol, Dept Bioinformat & Biosci, Islamabad Expressway,Kahuta Rd,Zone 5, Islamabad, Pakistan; [Ali, Sajid] Quaid E Azam Univ Islamabad & Prov TB Reference, Dept Microbiol, Lab Hayatabad Med Complex, Peshawar, Pakistan; [Masood, Nayyer; Afzal, Muhammad Tanvir] Capital Univ Sci & Technol, Dept Comp Sci, Islamabad, Pakistan; [Nadeem, Tariq] Univ Punjab, Natl Ctr Excellence Mol Biol, Lahore, Pakistan; [Khan, Anwar Sheed] Khyber Med Univ, Inst Basic Med Sci, Peshawar, Pakistan; [Khan, Anwar Sheed] Prov TB Control Lab, Hayatabad Med Complex Peshawar, Peshawar, Pakistan in 2019, Cited 39. Product Details of 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

BackgroundPyrazinamide (PZA) is an important component of first-line drugs because of its distinctive capability to kill subpopulations of persistent Mycobacterium tuberculosis (MTB). The prodrug (PZA) is converted to its active form, pyrazinoic acid (POA) by MTB pncA-encoded pyrazinamidase (PZase). Mutation in pncA is the most common and primary cause of PZA resistance. The aim of the present study was to explore the molecular characterization of PZA resistance in a Pashtun-dominated region of Khyber Pakhtunkhwa, Pakistan.MethodsWe performed drug susceptibility testing (DST) on 753 culture-positive isolates collected from the Provincial Tuberculosis Control Program Khyber Pakhtunkhwa using the BACTEC MGIT 960 PZA method. In addition, the pncA gene was sequenced in PZA-resistant isolates, and PZA susceptibility testing results were used to determine the sensitivity and specificity of pncA gene mutations.ResultsA total of 69 isolates were PZA resistant (14.8%). Mutations were investigated in 69 resistant, 26 susceptible and one H37Rv isolates by sequencing. Thirty-six different mutations were identified in PZA-resistant isolates, with fifteen mutations, including 194_203delCCTCGTCGTG and 317_318delTC, that have not been reported in TBDRM and GMTV Databases and previous studies. Mutations Lys96Thr and Ser179Gly were found in the maximum number of isolates (n=4 each). We did not detect mutations in sensitive isolates, except for the synonymous mutation 195C>T (Ser65Ser). The sensitivity and specificity of the pncA sequencing method were 79.31% (95% CI, 69.29 to 87.25%) and 86.67% (95% CI, 69.28 to 96.24%).ConclusionMutations in the pncA gene in circulating isolates of geographically distinct regions, especially in high-burden countries, should be investigated for better control and management of drug-resistant TB. Molecular methods for the investigation of PZA resistance are better than DST.

Product Details of 98-97-5. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Khan, MT; Malik, SI; Ali, S; Masood, N; Nadeem, T; Khan, AS; Afzal, MT or concate me.

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

SDS of cas: 98-97-5. I found the field of Chemistry; Crystallography very interesting. Saw the article Exploration of relative pi-electron localization in naphthalene aromatic rings by C-HMIDLINE HORIZONTAL ELLIPSIS pi interactions: experimental evidence, computational criteria, and database analysis published in 2019, Reprint Addresses Salimi, A (corresponding author), Ferdowsi Univ Mashhad, Fac Sci, Dept Chem, Mashhad, Iran.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

Based on the crystal engineering concept, four new esters containing alpha and beta-substituted naphthalene rings were designed, synthesized and fully characterized. The crystal structure analysis of the designed molecules revealed that the C-H-based interactions especially C-HMIDLINE HORIZONTAL ELLIPSIS pi have a significant role in the stabilization of crystal architectures. Regarding the molecular structure of naphthalene rings, one can find that bond lengths are divided into two groups (shorter and longer) so that relative localization is likely to occur in this system. Since pi-electron localization in aromatic rings has been previously introduced as responsible for stronger pi-stacking, this issue was investigated through C-HMIDLINE HORIZONTAL ELLIPSIS pi interaction in this study. Cambridge Structural Database (CSD) analysis was performed by exploration of suitable geometries for C-HMIDLINE HORIZONTAL ELLIPSIS pi(c) and C-HMIDLINE HORIZONTAL ELLIPSIS pi(e) in naphthalene and phenol systems (pi(c) and pi(e) are the centre and edge of the aromatic rings, respectively). The tendency factor (TF) of the C-H moiety toward ring bonds as a new CSD-based criterion was used to detect some of the resonance forms in aromatic rings. The results indicated that C-HMIDLINE HORIZONTAL ELLIPSIS pi(e) is a ubiquitous interaction which can be employed as an experimental probe for the detection of pi-localization in naphthalene rings. Systematic experimental studies, structural evidence and computational results on the title compounds confirmed the relative pi-electron localization, as well.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Samie, A; Salimi, A; Garrison, JC or concate me.. SDS of cas: 98-97-5

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

SDS of cas: 98-97-5. In 2020 J COORD CHEM published article about COMPLEXES; AZIDO; MN in [Yang, Zongfei; Yang, Xindi; Jin, Linyu; Dong, Kaili; Ma, Pengtao; Niu, Jingyang; Wang, Jingping] Henan Univ, Henan Key Lab Polyoxometalate Chem, Inst Mol & Crystal Engn, Coll Chem & Chem Engn, Kaifeng 475004, Henan, Peoples R China in 2020, Cited 29. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A high-nuclearity nickel-substituted polyoxotungstate, Na6K5.5H4.5{[Ni-8(OH)(6)(H2O)(2)](CO3)(3)(SiW9O34)(2)}center dot 22H(2)O (1), has been obtained by the reaction of Na-10[alpha-SiW9O34]center dot 18H(2)O, Ni(NO3)(2)center dot 6H(2)O and K(2)CO(3)in aqueous solution and characterized by IR spectroscopy, single crystal X-ray diffraction, thermal gravimetric analysis and elemental analysis. Carbonate is not only used to adjust the pH of the solution, but also is a structure-stabilizing agent. The polyoxoanion {[Ni-8(OH)(6)(H2O)(2)](CO3)(3)(SiW9O34)(2)}(16-)(1a) can be regarded as two {[Ni-4(OH)(3)(H2O)](SiW9O34)} subunits connected by three carbonate groups, which represents the first polyanion containing an octanuclear nickel cluster based on trivacant Keggin-type polyoxotungstate {XW9} (X = heteroatom). The subunit {[Ni-4(OH)(3)(H2O)](SiW9O34)} can be viewed as a tetranuclear nickel cluster linked to a trivacant Keggin-type polyoxotungstate {SiW9O34}. Furthermore, magnetic measurements show that1exhibits antiferromagnetic interactions.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Yang, ZF; Yang, XD; Jin, LY; Dong, KL; Ma, PT; Niu, JY; Wang, JP or concate me.. SDS of cas: 98-97-5

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

Quality Control of Pyrazine-2-carboxylic acid. Reddyrajula, R; Dalimba, U in [Reddyrajula, Rajkumar; Dalimba, Udayakumar] Natl Inst Technol Karnataka, Dept Chem, Organ Chem Lab, Mangalore 575025, India published The bioisosteric modification of pyrazinamide derivatives led to potent antitubercular agents: Synthesis via click approach and molecular docking of pyrazine-1,2,3-triazoles in 2020, Cited 38. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Tuberculosis remains as a major public health risk which causes the highest mortality rate globally and an improved regimen is required to treat the drug-resistant strains. Pyrazinamide is a first-line antitubercular drug used in combination therapy with other anti-TB drugs. Herein, we describe the modification of pyrazinamide structure using bioisosterism and rational approaches by incorporating the 1,2,3-triazole moiety. Three sets of pyrazine-1,2,3-triazoles (3a-o, 5a-o and 9a-l) are designed, synthesized and evaluated for their in vitro inhibitory potency against mycobacterium tuberculosis H(37)Rv. The pyrazine-1,2,3-triazoles synthesized through the bioisosteric modification displayed improved activity as compared to rationally modified pyrazine-1,2,3-triazoles. Among 42 title compounds, seven derivatives demonstrated significant anti-tubercular activity with the MIC of 1.56 mu g/mL, which are two-fold more potent than the parent compound pyrazinamide. Further, the synthesized pyrazinamide analogs demonstrated moderate inhibition activity against several bacterial strains and possessed an acceptable in vitro cytotoxicity profile as well. Additionally, the activity profile of pyrazine-1,2,3-triazoles was validated by performing the molecular docking studies against the Inh A enzyme. Furthermore, in silico ADME prediction revealed good oral bioavailability for the potent molecules.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Reddyrajula, R; Dalimba, U or concate me.. Quality Control of Pyrazine-2-carboxylic acid

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

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Synthesis of pyrazinamide analogues and their antitubercular bioactivity published in 2020. Recommanded Product: 98-97-5, Reprint Addresses Santoso, M (corresponding author), Inst Teknol Sepuluh Nopember, Fac Sci, Dept Chem, Kampus ITS Sukolilo, Surabaya 60111, Indonesia.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

The Yamaguchi reaction is widely and generally applied to synthesize esters and lactones. It involves 2,4,6-trichlorobenzoyl chloride as the Yamaguchi reagent, 4-dimethylaminopyridine, and triethylamine. Pyrazinamide is a crucial first-line drug for tuberculosis treatment, therefore their analogues are interesting in organic synthesis. In general, the synthesis pyrazinamide analogues involve reaction of pyrazine-2-carboxylic acids with thionyl chloride to yield the corresponding acyl chlorides, which on treatment with amines gave pyrazine-2-carboxamides. However, thionyl chloride is listed under the Chemical Weapons Convention and releases toxic sulfur oxide when react with carboxylic acid. We successfully synthesized series of pyrazinamide analogues using the Yamaguchi reaction. The synthesis involved reaction of pyrazine-2-carboxylic acid with various aliphatic and aromatic amines in the presence of Yamaguchi reagent and 4-dimethylaminopyridine. The yield of the pyrazine-2-carboxamides and the reaction time depended on the type of the amine (aliphatic vs aromatic), substitution pattern, and number of substituents on the aromatic amines.N-(4-chlorophenyl)pyrazine-2-carboxamides can be prepared by this method in 81% yield;N-(2-ethylhexyl)pyrazine-2-carboxamide andN-(4-fluorobenzyl)pyrazine-2-carboxamide showed the best activity againstMycobacterium tuberculosisH37Rv (<6.25 mu g/mL). This result could lead to find more active pyrazinamide analogues. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Wati, FA; Adyarini, PU; Fatmawati, S; Santoso, M or concate me.. Recommanded Product: 98-97-5

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

Recently I am researching about ACTIVATION, Saw an article supported by the NIA of the NIH [R01AG058673]; Alzheimer’s Drug Discovery Foundation [20150601]; Commonwealth of Virginia’s Alzheimer’s and Related Disease Research Award Fund [18-2]; NATIONAL INSTITUTE ON AGINGUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute on Aging (NIA) [R01AG058673] Funding Source: NIH RePORTER. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Jiang, YQ; He, L; Green, J; Blevins, H; Guo, CQ; Patel, SH; Halquist, MS; Mcrae, M; Venitz, J; Wang, XY; Zhang, SJ. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. Application In Synthesis of Pyrazine-2-carboxylic acid

NLRP3 inflammasomes have recently emerged as an attractive drug target for neurodegenerative disorders. In our continuing studies, a new chemical scaffold was designed as selective inhibitors of NLRP3 inflammasomes. Initial characterization of the lead HL16 demonstrated improved, however, nonselective inhibition on the NLRP3 inflammasome. Structure-activity relationship studies of HL16 identified a new lead, 17 (YQ128), with an IC50 of 0.30 +/- 0.01 mu M. Further studies from in vitro and in vivo models confirmed its selective inhibition on the NLRP3 inflammasome and its brain penetration. Furthermore, pharmacokinetic studies in rats at 20 mg/kg indicated extensive systemic clearance and tissue distribution, leading to a half-life of 6.6 h. However, the oral bioavailability is estimated to be only 10%, which may reflect limited GI permeability and possibly high first-pass effects. Collectively, these findings strongly encourage development of more potent analogues with improved pharmacokinetic properties from this new chemical scaffold.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Jiang, YQ; He, L; Green, J; Blevins, H; Guo, CQ; Patel, SH; Halquist, MS; Mcrae, M; Venitz, J; Wang, XY; Zhang, SJ or concate me.. Application In Synthesis of Pyrazine-2-carboxylic acid

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

Product Details of 98-97-5. In 2021 J MOL STRUCT 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. 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.

Product Details of 98-97-5. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Tomer, N; Goel, A; Ghule, VD; Malhotra, R or concate me.

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

Product Details of 98-97-5. Lei, M; Zhang, HY; Miao, H; Du, X; Zhou, H; Wang, J; Wang, XY; Feng, HY; Shi, JM; Liu, ZG; Shen, J; Zhu, YQ in [Lei, Meng; Miao, Hang; Feng, Huayun] Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Zhang, Haoyang; Du, Xiao; Zhou, Hui; Wang, Xueyuan; Zhu, Yongqiang] Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210046, Jiangsu, Peoples R China; [Wang, Jia; Shi, Jingmiao; Liu, Zhaogang; Zhu, Yongqiang] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, 9 Weidi Rd, Nanjing 210046, Jiangsu, Peoples R China; [Shen, Jian] Nanjing Normal Univ, Coll Chem & Mat Sci, 1 Wenyuan Rd, Nanjing 210046, Jiangsu, Peoples R China published Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors in 2019, Cited 21. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A series of novel tetrapeptidyl epoxyketone inhibitors of 20S proteasome was designed and synthesized. To fully understand the SAR, various groups at R-1, R-2, R-3, R-4 and R-5 positions, including aromatic and aliphatic substituents were designed, synthesized and biologically assayed. Based on the enzymatic results, seven compounds were selected to evaluate their cellular activities and soluble compound 36 showed strong potency against human multiple myeloma (MM) cell lines. Microsomal stability results indicated that compound 36 was more stable in mice, rat and human microsomes than marketed carfilzomib. The in vivo activities of this compound were evaluated with the xenograft mice models of MM cell lines ARH77 and RPMI-8226 with luciferase expression and the T/C value of the two models were 49.5% and 37.6%, respectively. To evaluate the potential cardiovascular toxicity, inhibition of hERG ion channel in HEK293 cells by compound 36 and carfilzomib was carried out. The results indicated that 36 had no binding affinity for the hERG ion channel while carfilzomib could bind it with IC50, of 92.1 mu M.

About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Lei, M; Zhang, HY; Miao, H; Du, X; Zhou, H; Wang, J; Wang, XY; Feng, HY; Shi, JM; Liu, ZG; Shen, J; Zhu, YQ or concate me.. Product Details of 98-97-5

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

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. Formula: C5H4N2O2. 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.

Formula: C5H4N2O2. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Yang, YJ; Wang, K; Yang, Y; Lai, FF; Chen, XG; Xiao, ZY or concate me.

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

SDS of cas: 98-97-5. Lei, M; Zhang, HY; Miao, H; Du, X; Zhou, H; Wang, J; Wang, XY; Feng, HY; Shi, JM; Liu, ZG; Shen, J; Zhu, YQ in [Lei, Meng; Miao, Hang; Feng, Huayun] Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Zhang, Haoyang; Du, Xiao; Zhou, Hui; Wang, Xueyuan; Zhu, Yongqiang] Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210046, Jiangsu, Peoples R China; [Wang, Jia; Shi, Jingmiao; Liu, Zhaogang; Zhu, Yongqiang] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, 9 Weidi Rd, Nanjing 210046, Jiangsu, Peoples R China; [Shen, Jian] Nanjing Normal Univ, Coll Chem & Mat Sci, 1 Wenyuan Rd, Nanjing 210046, Jiangsu, Peoples R China published Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors in 2019, Cited 21. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A series of novel tetrapeptidyl epoxyketone inhibitors of 20S proteasome was designed and synthesized. To fully understand the SAR, various groups at R-1, R-2, R-3, R-4 and R-5 positions, including aromatic and aliphatic substituents were designed, synthesized and biologically assayed. Based on the enzymatic results, seven compounds were selected to evaluate their cellular activities and soluble compound 36 showed strong potency against human multiple myeloma (MM) cell lines. Microsomal stability results indicated that compound 36 was more stable in mice, rat and human microsomes than marketed carfilzomib. The in vivo activities of this compound were evaluated with the xenograft mice models of MM cell lines ARH77 and RPMI-8226 with luciferase expression and the T/C value of the two models were 49.5% and 37.6%, respectively. To evaluate the potential cardiovascular toxicity, inhibition of hERG ion channel in HEK293 cells by compound 36 and carfilzomib was carried out. The results indicated that 36 had no binding affinity for the hERG ion channel while carfilzomib could bind it with IC50, of 92.1 mu M.

SDS of cas: 98-97-5. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Lei, M; Zhang, HY; Miao, H; Du, X; Zhou, H; Wang, J; Wang, XY; Feng, HY; Shi, JM; Liu, ZG; Shen, J; Zhu, YQ or concate me.

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