Category: Pyrazines

Application In Synthesis of Pyrazine-2-carboxylic acid. 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.

Welcome to talk about 98-97-5, If you have any questions, you can contact Yang, YJ; Wang, K; Yang, Y; Lai, FF; Chen, XG; Xiao, ZY or send Email.. Application In Synthesis of Pyrazine-2-carboxylic acid

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

An article Heterogeneous copper-catalyzed C-S coupling via insertion of sulfur dioxide: A novel and regioselective approach for the synthesis of sulfur-containing compounds WOS:000474675100001 published article about ONE-POT SYNTHESIS; H FUNCTIONALIZATION; ACTIVATION; SULFONYLATION; C(SP(2))-H; SODIUM in [Han, Junfen; Wang, Kai; You, Guirong; Wang, Guodong; Sun, Jian; Duan, Guiyun; Xia, Chengcai] Shandong First Med Univ & Shandong Acad Med Sci, Coll Pharm, Tai An 271000, Shandong, 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. Application In Synthesis of Pyrazine-2-carboxylic acid

A novel and regioselective protocol for C-S coupling of naphthylamines via the insertion of sulfur dioxide was developed by employing a heterogeneous copper catalyst, providing desired products in moderate to good yields. This strategy gives a powerful tool for the efficient preparation of sulfur-containing compounds. Control experiments declared that a single-electron transfer mechanism (SET) is responsible for this C-S cross coupling reaction.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Han, JF; Wang, K; You, GR; Wang, GD; Sun, J; Duan, GY; Xia, CC or send Email.

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

An article Pantoprazole Derivatives: Synthesis, Urease Inhibition Assay and In Silico Molecular Modeling Studies WOS:000528045700025 published article about HELICOBACTER-PYLORI; BIOISOSTERIC TRANSFORMATIONS; TRIPLE THERAPY; PATHOGENESIS; METAANALYSIS; OXADIAZOLES; PREDICTION in [Azizian, Homa] Iran Univ Med Sci, Sch Pharm, Dept Med Chem, Int Campus, Tehran, Iran; [Esmailnejad, Atefeh; Fathi Vavsari, Vaezeh; Balalaie, Saeed] KN Toosi Univ Technol, Peptide Chem Res Ctr, POB 15875-4416, Tehran, Iran; [Mahernia, Shabnam; Amanlou, Massoud] Univ Tehran Med Sci, TIPS, Drug Design & Dev Res Ctr, Tehran, Iran; [Balalaie, Saeed] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran in 2020, Cited 42. Application In Synthesis 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 number of pantoprazole derivatives were synthesized and screened for their urease inhibitory properties. Some of them showed potent inhibitions against jack bean urease. All compounds showed varying degree of IC50 in the range of 25.85 to 181 mu Mol as compared to standard acetohydroxamic acid (AHA) (100 +/- 2.02 mu Mol). Derivatives bearing 5-aryl-1,3,4-oxadiazole ring substitutions (aryl= pyrazyl, pyridyl and phenyl) were found to be more potent inhibitors than AHA and pantoprazole. The most promising compound, 2-((3,4-dimethoxypyridin-2-yl)methylthio)-5-(pyrazin-2-yl)-1,3,4-oxadiazole 12, with IC50 value of 25.85 +/- 1.21 showed remarkable urease inhibition activity. In silico molecular modeling investigation performed to rationalize the possible binding interaction and ADME properties of compounds over the active site of urease enzyme. The induced fit docking study showed that compound 12 interacted with conserved residues His593 and Arg609 located at the mouth of the urease active site flap and are essential for enzyme catalytic activity. These target compounds could be further studied as a lead skeleton for discovery of novel urease inhibitors.

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

Recently I am researching about IN-VITRO; MITOCHONDRIAL; CISPLATIN; DNA; LIGANDS; CYTOTOXICITY; MECHANISMS; CRYSTAL; DAMAGE; CELLS, Saw an article supported by the Key Scientific Research Project of Colleges and Universities in Henan Province [19A150017]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21371046, 21401041]; Funding Program for Academic Technology Leaders of the He’nan University of Urban Construction [YCJXSJSDTR201705]. Published in ELSEVIER SCIENCE INC in NEW YORK ,Authors: Li, S; Zhao, JA; Guo, Y; Mei, YM; Yuan, BP; Gan, N; Zhang, JS; Hu, JY; Hou, HW. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. SDS of cas: 98-97-5

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.

SDS of cas: 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Li, S; Zhao, JA; Guo, Y; Mei, YM; Yuan, BP; Gan, N; Zhang, JS; Hu, JY; Hou, HW or send Email.

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

An article Design, synthesis, and biological evaluation of tetrahydroisoquinoline-based diaryl urea derivatives for suppressing VEGFR-2 signaling WOS:000466009600010 published article about INHIBITORS; DISCOVERY; POTENT; ANGIOGENESIS; SAR in [Huang, Yuanzheng; Zhang, Yang; Li, Jiaming; Ma, Xiaodong; Hu, Mengqi; Yang, Yu; Gao, Sufan] Anhui Acad Chinese Med, Sch Pharm, Dept Pharmaceut Chem, Hefei, Anhui, Peoples R China; [Li, Jiaming; Ma, Xiaodong] Anhui Acad Chinese Med, Dept Med Chem, Hefei, Anhui, Peoples R China in 2019, Cited 18. 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

A novel structural series of tetrahydroisoquinoline-based compounds that incorporate the diaryl urea moiety was designed, synthesized, and biologically evaluated as suppressors of VEFGR-2 signaling. As a consequence, compounds 9k and 9s exhibited comparable or superior cytotoxic activity to that of gefitinib against the tested three cell lines, including A549, MCF-7, and PC-3. Importantly, both of them downregulated the expression of VEGFR-2, and inhibited VEGFR-2 phosphorylation at the concentration of 0.5 or 1.0 mu mol/ l. Besides, they suppressed human umbilical vein endothelial cell tube formation at the concentration of 4.0 mu mol/ l. Considering their capability of down-regulating VEGFR-2 expression and inhibiting VEGFR-2 phosphorylation, 9k and 9s may serve as suppressors of angiogenesis for further investigation. Copyright (c) 2018 Wolters Kluwer Health, Inc. All rights reserved.

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Huang, YZ; Zhang, Y; Li, JM; Ma, XD; Hu, MQ; Yang, Y; Gao, SF or send Email.

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

Recently I am researching about ACTIVATED CARBONS; PEROXIDATIVE OXIDATION; SURFACE-CHEMISTRY; II COMPLEX; ADSORPTION; IRON; IRRADIATION; IBUPROFEN; REMOVAL; ALKANES, Saw an article supported by the Fundacao para a Ciencia e Tecnologia (FCT), PortugalPortuguese Foundation for Science and Technology [UID/QUI/00100/2019, PTDC/QEQ-ERQ/1648/2014, UID/MULTI/00612/2019]; FCTPortuguese Foundation for Science and TechnologyEuropean Commission [SFRH/BPD/86693/2012]. Published in ELSEVIER in AMSTERDAM ,Authors: Andrade, MA; Mestre, AS; Carvalho, AP; Pombeiro, AJL; Martins, LMDRS. 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

The C-scorpionate iron(II) complex [FeCl2(Tpm)] [Tpm = kappa(3)-HC(C3H3N2)(3)] was immobilized on three nanoporous carbon supports to produce active, selective and recyclable catalysts for the oxidation of cyclohexane. The influence of the porous carbon supports on the performance of the heterogenized [FeCl2(Tpm)] catalyst was investigated using materials with distinct porosity: microporous (GL50-ox, wet oxidized GL50 Norit sample, and S, sisal-derived activated carbon prepared by chemical activation), and mesoporous (CMK-3) materials. The heterogenized systems exhibited good activity and rather high selectivity to the formation of KA (ketone-alcohol) oil (cyclohexanol and cyclohexanone mixture) from microwave-assisted oxidation of cyclohexane, and allowed their easy recovery and reuse, at least for four consecutive cycles. The most important outcome of this work was the significant self-catalytic activity observed for the pristine carbon materials GL50-ox and CMK-3 towards cyclohexane oxidation under Microwave irradiation, in the absence of the iron complex.

Application In Synthesis of 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 crystal structures of the ligand N-(quinolin-8-yl) pyrazine-2-carboxamide and of a tetranuclear copper(II) complex WOS:000477632400011 published article about CU-II COMPLEX; MOLECULAR-STRUCTURE; MAGNETIC-PROPERTIES in [Cati, Dilovan S.] Debiopharm Int SA, Chemin Messidor 5-7,CP 5911, CH-1002 Lausanne, Switzerland; [Stoeckli-Evans, Helen] Univ Neuchatel, Inst Phys, Rue Emile Argand 11, CH-2000 Neuchatel, Switzerland in 2019, Cited 31. 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

The title tridentate ligand, C14H10N4O, N-(quinolin-8-yl) pyrazine-2-carboxamide (HL1), crystallizes with three independent molecules (A, B and C) in the asymmetric unit. All three molecules are relatively planar (r.m.s. deviations are 0.068, 0.055 and 0.06 angstrom, respectively), with the NH H atom forming three-centered (bifurcated) intramolecular N-H center dot center dot center dot N hydrogen bonds in each molecule. There is also an intramolecular C-H center dot center dot center dot O contact present in each molecule, involving the benzene ring of the quinoline unit and the amide carboxamide O atom. In the crystal, the three molecules stack in columns with the various molecules being linked by offset pi-pi interactions [intercentroid distances vary from 3.367 (5) to 3.589 (5) angstrom], forming layers parallel to the ab plane. The title complex, [Cu-4(C42H44N8O16)]center dot 2CH(3)OH, {hexa-mu-acetato-1: 2 kappa O-2:O’;2:3 kappa O-8:O’;3:4 kappa O-2:O’-dimethanol-1 kappa O, 2 kappa O-bis[N-(quinolin-8-yl) pyrazine-2-carboxamide]-1 kappa N-3, N’, N ”; 4 kappa(3) N, N’, N ”-tetracopper(II) methanol disolvate} (I), was obtained by the reaction of HL1 with Cu(CH3CO2)(2). It consists of a tetranuclear complex with a central tetrakis(mu-acetato) dicopper paddle-wheel moiety linked on either side via bridging acetato ions to a mononuclear copper(II)-(L1) complex; it crystallizes as a methanol disolvate. The complex possesses inversion symmetry, being located about a center of symmetry situated at the mid-point of the Cu center dot center dot center dot Cu bond of the paddle-wheel moiety. In the crystal, the complex molecules are linked by O-H center dot center dot center dot O hydrogen bonds, forming chains along the [01 (1) over bar] direction, which are linked by offset pi-pi interactions [intercentroid distance = 3.7367 (11) angstrom] and C-H center dot center dot center dot O hydrogen bonds, leading to the formation of a supramolecular framework.

Safety of 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

Safety of Pyrazine-2-carboxylic acid. In 2019 J MED CHEM published article about ACTIVATION in [Jiang, Yuqi; He, Liu; Green, Jakob; Blevins, Hallie; Zhang, Shijun] Virginia Commonwealth Univ, Dept Med Chem, Richmond, VA 23298 USA; [Guo, Chunqing; Wang, Xiang-Yang] Virginia Commonwealth Univ, Dept Human & Mol Genet, Richmond, VA 23298 USA; [Patel, Sulay Harsiddhbhai; McRae, MaryPeace] Virginia Commonwealth Univ, Dept Pharmacotherapy & Outcomes, Richmond, VA 23298 USA; [Halquist, Matthew S.; Venitz, Jurgen] Virginia Commonwealth Univ, Dept Pharmaceut, Richmond, VA 23298 USA; [Jiang, Yuqi] Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Shandong, Peoples R China in 2019, Cited 30. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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.

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, 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 send Email.

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 Identification of Substituted Amino Acid Hydrazides as Novel Anti-Tubercular Agents, Using a Scaffold Hopping Approach published in 2020. Computed Properties of C5H4N2O2, Reprint Addresses Sellars, JD (corresponding author), Newcastle Univ, Biosci Inst, Fac Med Sci, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.; Sellars, JD (corresponding author), Fac Med Sci, Sch Pharm, King George VI Bldg, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Discovery and development of new therapeutic options for the treatment of Mycobacterium tuberculosis (Mtb) infection, particularly drug-resistant strains, are urgently required to tackle the global burden of this disease. Herein, we reported the synthesis of a novel series of N-substituted amino acid hydrazides, utilising a scaffold hopping approach within a library of anti-tubercular agents. Efficacy and selectivity were evaluated against three strains of Mtb (wild-type, isoniazid-resistant and rifampicin-resistant), and cytotoxicity against macrophages in vitro. The antibacterial activity and therapeutic index of these molecules were significantly affected by modifications with the N-substituents. Introduction of a 3,5-dinitroaryl moiety demonstrated enhanced antibacterial activity against all three strains of Mtb. In contrast, the inclusion of an imidazo [1,2-a]pyridine-3-carboxy moiety resulted in enhanced activity towards isoniazid mono-resistant Mtb relative to wild-type Mtb. Consequently, this scaffold hopping approach showed significant promise for exemplification of novel molecules with specific activity profiles against drug-resistant tuberculosis.

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

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. 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

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.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Khan, MT; Malik, SI; Ali, S; Masood, N; Nadeem, T; Khan, AS; Afzal, MT or send Email.

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