Month: December 2021

An article Synthesis, characterization, pharmacological and computational studies of 4, 5, 6, 7-tetrahydro-1, 3-benzothiazole incorporated azo dyes WOS:000456491500070 published article about AB-INITIO CALCULATIONS; SPECTROSCOPIC FT-IR; MOLECULAR DOCKING; VIBRATIONAL-SPECTRA; DNA-BINDING; CRYSTAL-STRUCTURE; DFT CALCULATIONS; DISPERSE DYES; MYCOBACTERIUM-TUBERCULOSIS; ANTIMICROBIAL PROPERTIES in [Maliyappa, M. R.; Keshavayya, J.; Mallikarjuna, N. M.] Kuvempu Univ, Dept PG Studies & Res Chem, Shimoga 577451, Karnataka, India; [Krishna, P. Murali; Shivakumara, N.] MS Ramaiah Inst Technol, Dept Chem, Bengaluru 560054, India; [Sandeep, Telkar] Kuvempu Univ, Dept PG Studies & Res Biotechnol & Bioinformat, Shimoga 577451, Karnataka, India; [Sailaja, Krishnamurty] Natl Chem Lab, Phys & Mat Chem Div, Pune 411008, Maharashtra, India; [Nazrulla, Mohammed Azeezulla] CSIR Cent Electrochem Res Inst, Funct Mat Div, Karaikkudi 630006, Tamil Nadu, India in 2019, Cited 82. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

The present work describes the synthesis of five novel heterocyclic azo dyes (4a-4e) through conventional diazo-coupling reaction of 4, 5, 6, 7-tetrahydro-1, 3-benzothiazole with various coupling compounds at 0-5 degrees C. The chemical structures of the synthesized azo dyes were characterized by both theoretical and experimental techniques. All the synthesized molecules were evaluated for their antioxidant activity by two different techniques such as DPPH and FRAP. The results indicated that all the synthesized compounds proved to be potent antioxidants. The anti-mycobacterial activity of the azo dyes was tested against M. tuberculosis and the compounds 4a and 4e showed higher activity among the tested dyes. The DNA binding studies showed effective intercalation properties between the azo dyes and CT-DNA. Finally, the molecular docking studies indicated a possible interaction of the azo dyes with target receptor RpsA. (C) 2018 Elsevier B.V. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Maliyappa, MR; Keshavayya, J; Mallikarjuna, NM; Krishna, PM; Shivakumara, N; Sandeep, T; Sailaja, K; Nazrulla, MA or send Email.. Formula: C5H4N2O2

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. HPLC of Formula: C5H4N2O2. 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.

HPLC of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Reddyrajula, R; Dalimba, U or send Email.

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

Safety of Pyrazine-2-carboxylic acid. Authors Korff, M; Imberg, L; Will, JM; Buckreiss, N; Kalinina, SA; Wenzel, BM; Kastner, GA; Daniliuc, CG; Barth, M; Ovsepyan, RA; Butov, KR; Humpf, HU; Lehr, M; Panteleev, MA; Poso, A; Karst, U; Steinmetzer, T; Bendas, G; Kalinin, DV in AMER CHEMICAL SOC published article about in [Korff, Marvin; Imberg, Lukas; Kastner, Gregor A.; Barth, Maximilian; Lehr, Matthias; Kalinin, Dmitrii, V] Univ Munster, Inst Pharmaceut & Med Chem, D-48149 Munster, Germany; [Will, Jonas M.; Karst, Uwe] Univ Munster, Inst Inorgan & Analyt Chem, D-48149 Munster, Germany; [Bueckreiss, Nico; Bendas, Gerd] Univ Bonn, Pharmaceut Inst, D-53121 Bonn, Germany; [Kalinina, Svetlana A.; Humpf, Hans-Ulrich] Univ Munster, Inst Food Chem, D-48149 Munster, Germany; [Wenzel, Benjamin M.; Steinmetzer, Torsten] Philipps Univ Marburg, Inst Pharmaceut Chem, Dept Pharm, D-35032 Marburg, Germany; [Daniliuc, Constantin G.] Univ Munster, Inst Organ Chem, D-48149 Munster, Germany; [Ovsepyan, Ruzanna A.; Butov, Kirill R.; Panteleev, Mikhail A.] Dmitriy Rogachev Natl Med Res Ctr Pediat Hematol, Lab Translat Med, Moscow 117997, Russia; [Ovsepyan, Ruzanna A.; Butov, Kirill R.; Panteleev, Mikhail A.] Russian Acad Sci, Ctr Theoret Problems Physicochem Pharmacol, Moscow 119991, Russia; [Panteleev, Mikhail A.] Lomonosov Moscow State Univ, Fac Phys, Moscow 119991, Russia; [Panteleev, Mikhail A.] Moscow Inst Phys & Technol, Fac Biol & Med Phys, Dolgoprudnyi 141700, Russia; [Poso, Antti] Univ Eastern Finland, Fac Hlth Sci, Sch Pharm, Kuopio 70211, Finland; [Poso, Antti] Univ Hosp Tubingen, Dept Internal Med 8, D-72076 Tubingen, Germany in 2020, Cited 75. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

We herein report the conventional and microscale parallel synthesis of selective inhibitors of human blood coagulation factor XIIa and thrombin exhibiting a 1,2,4-triazol-5-amine scaffold. Structural variations of this scaffold allowed identifying derivative 21i, a potent 29 nM inhibitor of FXIIa, with improved selectivity over other tested serine proteases and also finding compound 21m with 27 nM inhibitory activity toward thrombin. For the first time, acylated 1,2,4-triazol-5-amines were proved to have anticoagulant properties and the ability to affect thrombin- and cancer-cell-induced platelet aggregation. Performed mass spectrometric analysis and molecular modeling allowed us to discover previously unknown interactions between the synthesized inhibitors and the active site of FXIIa, which uncovered the mechanistic details of FXIIa inhibition. Synthesized compounds represent a promising starting point for the development of novel antithrombotic drugs or chemical tools for studying the role of FXIIa and thrombin in physiological and pathological processes.

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

In 2020 ASIAN J ORG CHEM published article about CROSS-COUPLING REACTIONS; CARBOXYLIC-ACIDS; QUINOLINE; SITE; DERIVATIVES; CARBONYLATION; COMPLEXES; RECEPTOR in [Hu, Jingyan; Ye, Xiefeng; Hao, Shuai; Zhao, Qianrui; Zhao, Mingqin; Wei, Yuewei; Wu, Zhiyong; Ji, Xiaoming] Henan Agr Univ, Flavors & Fragrance Engn & Technol Res Ctr Henan, Coll Tobacco Sci, 95 Wenhua Rd, Zhengzhou 450002, Peoples R China; [Wang, Na] China Tobacco Hubei Ind Co Ltd, Ctr Technol, 1355 Jinshan Rd, Wuhan 430040, Peoples R China in 2020, Cited 46. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. HPLC of Formula: C5H4N2O2

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogues via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides has been developed. The reaction proceeds efficiently under simple reaction conditions and features the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

HPLC of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Hu, JY; Ye, XF; Hao, S; Zhao, QR; Zhao, MQ; Wei, YW; Wu, ZY; Wang, N; Ji, XM or send Email.

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

Recently I am researching about PHASE-II TRIAL; ORGANIC SULFUR CHEMISTRY; QUINOXALINE ANTIBIOTICS; TRIOSTIN; HYPOXIA; DESULFURIZATION; DEPSIPEPTIDES; QUINOMYCIN; PATHWAY, Saw an article supported by the JSPSMinistry of Education, Culture, Sports, Science and Technology, Japan (MEXT)Japan Society for the Promotion of Science [16H05097, 19H03345, 18H04599, 20H04757]; Hokkaido University, Global Facility Center (GFC), Pharma Science Open Unit (PSOU) – MEXT under Support Program for Implementation of New Equipment Sharing System, Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Suppor [18am0101093j0002]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Kojima, K; Yakushiji, F; Katsuyama, A; Ichikawa, S. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. Recommanded Product: Pyrazine-2-carboxylic acid

The first total synthesis of echinomycin (1) was accomplished by featuring the late-stage construction of the thioacetal moiety via Pummerer rearrangement and simultaneous cyclization, as well as two-directional elongation of the peptide chains to construct a C2-symmetrical bicyclic octadecadepsipeptide bridged with a sulfide linkage. This strategy can be applicable to a variety of echinomycin analogues.

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.. Recommanded Product: 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 Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo published in 2020. Name: Pyrazine-2-carboxylic acid, Reprint Addresses Bao, R; Luo, YF (corresponding author), Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.; Bao, R; Luo, YF (corresponding author), Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

Welcome to talk about 98-97-5, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or send Email.. Name: Pyrazine-2-carboxylic acid

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.

Safety of Pyrazine-2-carboxylic acid. 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.

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. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

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.. Formula: C5H4N2O2

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

Recently I am researching about FLUORESCENT DETECTION; CHEMOSENSOR; PROBE; COPPER; PRECONCENTRATION; FE3+; SITE, Saw an article supported by the UGC-JRF from UGC, New Delhi [169(June 2018)/2019(NET/CSIR), 264/(CSIR-UGC NET JUNE 2018)]. Product Details of 98-97-5. Published in ELSEVIER in AMSTERDAM ,Authors: Tomer, N; Goel, A; Ghule, VD; Malhotra, R. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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. 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

Name: Pyrazine-2-carboxylic acid. Recently I am researching about DRUG-RESISTANCE; GENE; SUSCEPTIBILITY; PREVALENCE; RPSA, Saw an article supported by the . Published in BMC in LONDON ,Authors: Khan, MT; Malik, SI; Ali, S; Masood, N; Nadeem, T; Khan, AS; Afzal, MT. The CAS is 98-97-5. Through research, I have a further understanding and discovery 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.

Name: 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