Category: 98-97-5

Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P in [Sun, Qi; Zhou, Tongliang; Xi, Dandan; Li, Xiaona; Lu, Zirui; Xu, Fengrong; Wang, Chao; Niu, Yan; Xu, Ping] Peking Univ, Sch Pharmaceut Sci, Dept Med Chem, Hlth Sci Ctr, Beijing 100191, Peoples R China; [Sun, Qi] Peking Univ, Coll Chem & Mol Engn, State Key Lab Struct Chem Unstable & Stable Speci, BNLMS, Beijing 100871, Peoples R China published Design and synthesis of tripeptidyl furylketones as selective inhibitors against the beta 5 subunit of human 20S proteasome in 2020, Cited 31. Safety 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 series of tripeptidic proteasome inhibitors with furylketone as C-terminus were designed and synthesized. Biochemical evaluations against beta 1, beta 2 and beta 5 subunits revealed that they acted selectively on beta 5 subunit with IC(50)s against chymotrypsin-like (CT-L) activity in micromolar range. LC-MS/MS analysis of the ligand-20S proteasome mixture showed that the most potent compound 11m (IC50 = 0.18 mu M) made no covalent modification on 20S proteasome. However, it was identified acting in a slowly reversible manner in wash-out assay and the reversibility was much lower than that of MG132, suggesting the possibility of these tripeptidic furylketones forming reversible covalent bonds with 20S proteasome. Several compounds were selected for anti-proliferative assay towards multiple cancer cell lines, and compound 11m displayed comparable potency to positive control (MG132) in all cell lines tested. Furthermore, the pharmacokinetic (PK) data in rats indicated 11m behaved similarly (C-max, 2007 mu g/L; AUC(0-t), 680 mu g/L.h; V-ss, 0.66 L/kg) to the clinical used agent carfilzomib. All these data suggest 11m is a good lead compound to be developed to novel anti-tumor agent. (c) 2020 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P or send Email.. Safety of Pyrazine-2-carboxylic acid

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

Authors Priyanka; Neelabh; Tiwari, N; Sharma, RK; Gupta, P; Misra, S; Misra-Bhattacharya, S; Butcher, RJ; Singh, K; Katiyar, D in WILEY-V C H VERLAG GMBH published article about PARASITIC NEMATODE; CHITINASE; COUMARINS; DRUG in [Priyanka; Tiwari, Neha; Sharma, Rajesh K.; Katiyar, Diksha] Banaras Hindu Univ, Dept Chem, MMV, Varanasi 221005, Uttar Pradesh, India; [Neelabh; Singh, Karuna] Banaras Hindu Univ, Dept Zool, MMV, Varanasi 221005, Uttar Pradesh, India; [Gupta, Poonam] Mahanand Miss Harijan Coll, Dept Chem, Ghaziabad 201001, India; [Misra, Sweta; Misra-Bhattacharya, Shailja] CSIR, Cent Drug Res Inst, Div Parasitol, BS 10-1,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India; [Butcher, Ray J.] Howard Univ, Dept Chem, 525 Coll St NW, Washington, DC 20059 USA in 2019, Cited 28. Computed Properties of C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A series of 7-benzamidocoumarin derivatives 10-25 starting from 7-amino coumarins 7 and 8 has been synthesized, characterized and evaluated in vitro for antifilarial activity against the human lymphatic filarial parasite, Brugia malayi. Compounds 13 and 20-23 showed permanent paralysis of the worm with 90-95% inhibition of motility of adult worms at 10 mu M. All the synthesized compounds were docked on the modeled receptor of Onchocerca volvulus chitinase OvCHT1. Compound 13 with binding energy of -7.95 Kcal/mol showing three hydrogen bonds with the active site of the enzyme emerged as the best inhibitor.

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

Formula: C5H4N2O2. In 2020 MED CHEM RES published article about ANTIMYCOBACTERIAL EVALUATION; ONE-POT; ESTERIFICATION; ESTERS; AMIDES; AMINES in [Wati, First A.; Adyarini, Prisna U.; Fatmawati, Sri; Santoso, Mardi] Inst Teknol Sepuluh Nopember, Fac Sci, Dept Chem, Kampus ITS Sukolilo, Surabaya 60111, Indonesia in 2020, Cited 24. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

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. Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Wati, FA; Adyarini, PU; Fatmawati, S; Santoso, M or send Email.

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

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. Application In Synthesis of Pyrazine-2-carboxylic acid

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

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

Computed Properties of C5H4N2O2. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Population Pharmacokinetic Modelling of Pyrazinamide and Pyrazinoic Acid in Patients with Multi-Drug Resistant Tuberculosis published in 2019, Reprint Addresses Mugabo, P (corresponding author), Univ Western Cape, Sch Pharm, Private Bag X17, ZA-7535 Bellville, Cape Town, South Africa.. The CAS is 98-97-5. Through research, I have a further understanding and discovery 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.

Computed Properties of C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Mugabo, P; Mulubwa, M or send Email.

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

Zhao, HY; Wang, B; Fu, L; Li, G; Lu, HJ; Liu, YK; Sheng, L; Li, Y; Zhang, BX; Lu, Y; Ma, C; Huang, HH; Zhang, DF; Lu, Y 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 published Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis in 2020, Cited 30. 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.

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.

Welcome to talk about 98-97-5, If you have any questions, you can contact Zhao, HY; Wang, B; Fu, L; Li, G; Lu, HJ; Liu, YK; Sheng, L; Li, Y; Zhang, BX; Lu, Y; Ma, C; Huang, HH; Zhang, DF; Lu, Y or send Email.. Product Details of 98-97-5

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

Formula: C5H4N2O2. I found the field of Engineering; Materials Science; Physics very interesting. Saw the article Preparation of Fe-C nanofiber composites by metal organic complex and potential application in supercapacitors published in 2019, Reprint Addresses Han, LM (corresponding author), Inner Mongolia Univ Technol, Chem Engn Coll, Hohhot 010051, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

In this paper, high-capacity supercapacitor material (Fe-Nx/CNFs) synthesized by electrospinning a metal complex in PAN/DMF solution with different temperatures was presented. Moreover, nitrogen doping (N-doping in short) has been used to tailor the properties of carbon nanofibers and rendered its potential use for capacitor as an effective way. The structural and morphological properties of the Fe-Nx/CNFs were fully characterized and the carbonation temperature of the Fe-Nx/CNFs precursor was optimized. Compared with the pure carbon nanofiber, the annealing temperature of optimized Fe-Nx/CNFs composites electrode material was 550 degrees C. Fabricating the binder-free iron-based electrode exhibited a higher capacitance of 629Fg(-1) at the current density of 1Ag(-1) in 4molL(-1) aqueous KOH electrolyte. Meanwhile, a cycling stability of 97% capacitance retention after cycling 2500at 5Ag(-1) was maintained. This outstanding performance was attributed to the formation of the Fe-N bond and N-doped carbon nanofibers that effectively facilitates electronic transport. Therefore, carbon nanofibers, wherein nitrogen-doped metal (iron) center, exhibited high performance as supercapacitors.

Welcome to talk about 98-97-5, If you have any questions, you can contact Wang, GY; Sun, XW; Bai, J; Han, LM or send Email.. Formula: C5H4N2O2

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

An article Palladium-Catalyzed Regioselective C-H Iodination of Unactivated Alkenes WOS:000470939200020 published article about DIRECTING GROUPS; MOLECULAR I-2; BONDS; FUNCTIONALIZATION; HALOGENATION; ALKYLATION; C(SP(3))-H; ARYLATION; MILD; ALLYLAMINES in [Schreib, Benedikt S.; Carreira, Erick M.] Swiss Fed Inst Technol, HCI, Vladimir Prelog Weg 3, CH-8093 Zurich, Switzerland in 2019, Cited 63. Recommanded Product: 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A palladium-catalyzed C-H iodination of unactivated alkenes is reported. A picolinamide directing group enables the regioselective functionalization of a wide array of olefins to furnish iodination products as single stereoisomers. Mechanistic investigations suggest the reversible formation of a six-membered alkenyl palladacycle intermediate through a turnover-limiting C-H activation.

Welcome to talk about 98-97-5, If you have any questions, you can contact Schreib, BS; Carreira, EM or send Email.. Recommanded Product: 98-97-5

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

In 2019 ACTA CRYSTALLOGR E 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. COA of Formula: C5H4N2O2

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.

COA of Formula: C5H4N2O2. Welcome to talk about 98-97-5, If you have any questions, you can contact Cati, DS; Stoeckli-Evans, H or send Email.

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

An article Efficient synthesis of novel RGD based peptides and the conjugation of the pyrazine moiety to their N-terminus WOS:000459942300029 published article about ADHESION MOLECULE L1; CELL-ADHESION; INTEGRIN ALPHA(V)BETA(3); CYCLIC RGD; VITRONECTIN-RECEPTOR; MALIGNANT-MELANOMA; DISCOVERY; STRATEGIES; BINDING; DESIGN in [Hamdan, Fatima; Bigdeli, Zahra; Balalaie, Saeed] KN Toosi Univ Technol, Peptide Chem Res Ctr, POB 15875-4416, Tehran, Iran; [Balalaie, Saeed] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran; [Sewald, Norbert; Michalek, Carmela] Bielefeld Univ, Dept Chem, Organ & Bioorgan Chem, Univ Str 25, D-33615 Bielefeld, Germany in 2019, Cited 97. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. HPLC of Formula: C5H4N2O2

The synthesis of modified RGD peptides and their conjugation to the pyrazine skeleton at their N-terminus are described. To modify and alter the RGD sequence, short bioactive peptides such as FALKF and NGRG were added to the RGD N-terminus. Moreover, the in vitro investigation of these modified peptides, by a cell adhesion assay using the melanoma cell lines M21 expressing alpha(v)beta(3) and M21L lacking alpha(v) expression, was made and interestingly peptide 4 containing the pyrazine moiety with the linear RGDFAKLF sequence gave the best IC50 value with M21 and all the peptides were unable to bind to M21L, demonstrating the selective recognition to alpha(v)beta(3). The results showed pyrazine plays an essential role in the activity of the peptides. From these results, we can suggest that these peptides can affect cancer cells by abrogation of cell adhesion (cell migration).

Welcome to talk about 98-97-5, If you have any questions, you can contact Hamdan, F; Bigdeli, Z; Balalaie, S; Sewald, N; Michalek, C or send Email.. HPLC of Formula: C5H4N2O2

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