Month: November 2021

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

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.

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.. Safety 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 2020 BIOORG MED CHEM LETT published article about CYTOCHROME BC(1) COMPLEX; IRON-SULFUR PROTEIN; BC1 COMPLEX; DISCOVERY; SITE; FUNGICIDE; AMETOCTRADIN; RESISTANCE; MECHANISM; BINDING in [Cheng, Hua; Yang, Lu; Liu, Hong-Fu; Zhang, Rui] Hubei Univ Arts & Sci, Dept Chem Engn & Food Sci, Xiangyang 441053, Peoples R China; [Chen, Cheng] Wuhan Univ Technol, State Key Lab Adv Technol Mat Synth & Proc, Wuhan 430070, Peoples R China; [Wu, Yuan; Jiang, Wen] Cent China Normal Univ, Coll Chem, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China in 2020, Cited 47. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

Mitochondrial complex III is one of the most promising targets for a number of pharmaceuticals and fungicides. Due to the wide-spread use of complex III-inhibiting fungicides, a considerable increase of resistance has occurred worldwide. Therefore, inhibitors with novel scaffolds and potent activity against complex III are still in great demand. In this article, a new series of amide compounds bearing the diaryl ether scaffold were designed and prepared, followed by the biological evaluation. Gratifyingly, several compounds demonstrated potent activity against succinate-cytochrome c reductase (SCR, a mixture of mitochondrial complex II and complex III), with compound 3w possessing the best inhibitory activity (IC50 = 0.91 +/- 0.09 mu mol/L). Additional studies verified that 3w was a new inhibitor of complex III. Moreover, computational simulations elucidated that 3w should bind to the Q(o) site of complex III. We believe this work will be valuable for the preparation and discovery of more complex III inhibitors.

Product Details of 98-97-5. Welcome to talk about 98-97-5, If you have any questions, you can contact Cheng, H; Yang, L; Liu, HF; Zhang, R; Chen, C; Wu, Y; Jiang, W or send Email.

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

Recommanded Product: 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.

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

Authors Ying, J; Fu, LY; Zhong, GQ; Wu, XF in AMER CHEMICAL SOC published article about BASIC SIDE-CHAINS; C-H CARBONYLATION; OXIDATIVE CARBONYLATION; DESIGN; C(SP(2))-H; INHIBITORS; BONDS; OPTIMIZATION; CYCLIZATION; ACTIVATION in [Ying, Jun; Fu, Lu-Yang; Zhong, Guoqiang; Wu, Xiao-Feng] Zhejiang Sci Tech Univ, Dept Chem, Xiasha Campus, Hangzhou 310018, Peoples R China; [Wu, Xiao-Feng] Univ Rostock, Leibniz Inst Katalyse eV, Albert Einstein Str 29a, D-18059 Rostock, Germany in 2019, Cited 33. Category: Pyrazines. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

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.

Category: Pyrazines. 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

An article The bioisosteric modification of pyrazinamide derivatives led to potent antitubercular agents: Synthesis via click approach and molecular docking of pyrazine-1,2,3-triazoles WOS:000504873300052 published article about ANTI-TUBERCULAR ACTIVITY; DESIGN; HYBRIDS; 1,2,3-TRIAZOLE; HYBRIDIZATION; ANTIMYCOBACTERIAL; DIARYLQUINOLINE in [Reddyrajula, Rajkumar; Dalimba, Udayakumar] Natl Inst Technol Karnataka, Dept Chem, Organ Chem Lab, Mangalore 575025, India in 2020, Cited 38. Name: Pyrazine-2-carboxylic acid. 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.

Welcome to talk about 98-97-5, If you have any questions, you can contact Reddyrajula, R; Dalimba, U or send Email.. Name: Pyrazine-2-carboxylic acid

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

Recently I am researching about CORROSION-INHIBITORS; HYDROCHLORIC-ACID; CARBON-STEEL; BENZIMIDAZOLE DERIVATIVES; SCHIFF-BASES; PART II; ADSORPTION; BEHAVIOR; IODIDE; THIOSEMICARBAZONE, Saw an article supported by the Cukurova University Scientific Research Projects Coordination UnitCukurova University [FDK-2017-9860]; Mardin Artuklu UniversityMardin Artuklu University. Published in TAYLOR & FRANCIS LTD in ABINGDON ,Authors: Kelesoglu, A; Sigircik, G; Yildiz, R; Dehri, I. 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

Pyrazinecarboxylic acid (PCA) was examined as a potential corrosion inhibitor for mild steel (MS) in 0.5 M HCl environment. The methods of electrochemical impedance spectroscopy (EIS), linear polarization resistance (LPR), as well potentiodynamic (PD) polarization were utilized. Furthermore, atomic force microscopy (AFM) and quantum chemical calculations were utilized. PD polarization curves demonstrated that PCA exhibited mixed inhibitor behavior. Scanning electron microscopy (SEM) offered the creation of an adsorptive layer on the surface of MS which prevented the steel against corrosive specimens. Furthermore, density functional theory (DFT) presented good agreement with electrochemical experimental results. The adsorption equilibrium constant (k(ads)) value was calculated to be 3.704 x 10(4) M-1 which was related to a high proportion of inhibitor on the surface. In the presence of 1.0 mM PCA, inhibition efficiency was determined as 95.2% from EIS results.

Recommanded Product: 98-97-5. 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 Novel Homo-Bivalent and Polyvalent Compounds Based on Ligustrazine and Heterocyclic Ring as Anticancer Agents WOS:000507299600083 published article about SIGNALING PATHWAY; NATURAL-PRODUCTS; DERIVATIVES; APOPTOSIS; DESIGN; DISCOVERY; PREDICTION; CURCUMIN; ACID in [Wang, Jiawen; Liu, Tianjun] Tianjin Univ Tradit Chinese Med, Grad Inst, Tianjin 301617, Peoples R China; [Hong, Ge; Li, Guoliang; Wang, Wenzhi; Liu, Tianjun] Chinese Acad Med Sci & Peking Union Med Coll, Inst Biomed Engn, Tianjin Key Lab Biomed Mat, Tianjin 300192, Peoples R China; [Hong, Ge; Liu, Tianjun] 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 2019, Cited 30. 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

Bivalent and polyvalent inhibitors can be used as antitumor agents. In this experiment, eight ligustrazine dimers and seven ligustrazine tetramers linked by alkane diamine with different lengths of carbon chain lengths were synthesized. After screening their antiproliferation activities against five cancer cell lines, most ligustrazine derivatives showed better cytotoxicity than the ligustrazine monomer. In particular, ligustrazine dimer 8e linked with decane-1,10-diamine exhibited the highest cytotoxicity in FaDu cells with an IC50 (50% inhibiting concentration) value of 1.36 nM. Further mechanism studies suggested that 8e could induce apoptosis of FaDu cells through the depolarization of mitochondrial membrane potential and S-phase cell cycle arrest. Inspired by these results, twenty-seven additional small molecule heterocyclic dimers linked with decane-1,10-diamine and nine cinnamic acid dimers bearing ether chain were synthesized and screened. Most monocyclic and bicyclic aromatic systems showed highly selective anti-proliferation activity to FaDu cells and low toxicity to normal MCF 10A cells. The structure-activity relationship revealed that the two terminal amide bonds and the alkyl linker with a chain length of 8-12 carbon were two important factors to maintain its antitumor activity. In addition, the ADMET calculation predicted that most of the potent compounds had good oral bioavailability.

SDS of cas: 98-97-5. 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

Application In Synthesis of Pyrazine-2-carboxylic acid. Authors Guin, S; Dolui, P; Zhang, XL; Paul, S; Singh, VK; Pradhan, S; Chandrashekar, HB; Anjana, SS; Paton, RS; Maiti, D in WILEY-V C H VERLAG GMBH published article about in [Guin, Srimanta; Dolui, Pravas; Paul, Satyadip; Singh, Vikas Kumar; Pradhan, Sukumar; Chandrashekar, Hediyala B.; Anjana, S. S.; Maiti, Debabrata] Indian Inst Technol, Dept Chem, Mumbai 400076, Maharashtra, India; [Zhang, Xinglong; Paton, Robert S.] Univ Oxford, Chem Res Lab, Dept Chem, Mansfield Rd, Oxford OX1 3TA, England in 2019, Cited 72. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Directed C-H functionalization has been realized as a complementary tool to the traditional approaches for a straightforward access of non-proteinogenic amino acids; albeit such a process is restricted mostly up to the gamma-position. In the present work, we demonstrate the diverse (hetero) arylation of amino acids and analogous aliphatic amines selectively at the remote delta-position by tuning the reactivity controlled by ligands. An organopalladium delta-C(sp(3))-H activated intermediate has been isolated and crystallographically characterized. Mechanistic investigations carried out experimentally in conjunction with computational studies shed light on the difference in the mechanistic picture depending on the substrate structure.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Guin, S; Dolui, P; Zhang, XL; Paul, S; Singh, VK; Pradhan, S; Chandrashekar, HB; Anjana, SS; Paton, RS; Maiti, D or send Email.

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

In 2019 J PESTIC SCI published article about ACYL-COA; ASPERGILLUS-FUMIGATUS; CHEMICAL-MODIFICATION; STRUCTURE ELUCIDATION; INHIBITORS; POTENT; RESISTANCE; METABOLITE in [Guro, Kimihiko; Horikoshi, Ryo; Nakamura, Satoshi; Mitomi, Masaaki; Oyama, Kazuhiko] Meiji Seika Pharma Co Ltd, Agr & Vet Div, Agr & Vet Res Labs, Kohoku Ku, 760 Morooka Cho, Yokohama, Kanagawa, Japan; [Hirose, Tomoyasu; Sunazuka, Toshiaki; Omura, Satoshi] Kitasato Univ, Kitasato Inst Life Sci, Grad Sch Infect Control Sci, Tokyo, Japan in 2019, Cited 22. 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

Pyripyropene A (PP-A), a secondary metabolite produced by filamentous fungi, shows insecticidal activity against agricultural insect pests. Synthesized PP derivatives also show a narrow insecticidal spectrum but high insecticidal activities against such sucking pests. PP-A has a low eco-toxicological impact and satisfies a prerequisite for next-generation insecticides. We investigated the effects of conversion of the 3-pyridyl and a-pyrone rings to other rings, as well as the effects of esterification, dehydration, and oxidization at the C-13 position in natural PP analogues, on the insecticidal activity and spectrum. The conversions of the 3-pyridyl and alpha-pyrone rings markedly reduced the insecticidal activity with a minimal impact on the spectrum, indicative of an important role for these rings in insecticidal activity. Some derivatives with modified structures at the C-13 position showed a higher inhibitory effect on the motility of canine heartworms and mosquito vectors than did PP-A, suggesting their utility as filaria control drugs.

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Guro, K; Horikoshi, R; Nakamura, S; Mitomi, M; Oyama, K; Hirose, T; Sunazuka, T; Omura, S or send Email.

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