Month: January 2022

Application In Synthesis of Pyrazine-2-carboxylic acid. In 2020 J ORGANOMET CHEM published article about TRANSFER HYDROGENATION; ALPHA-ALKYLATION; RUTHENIUM(II) COMPLEXES; PRIMARY ALCOHOLS; KETONES; IRIDIUM; DEHYDROGENATION; REACTIVITY; SECONDARY; BEARING in [Pakyapan, Bilge; Kavukcu, Serdar Batikan; Turkmen, Hayati] Univ Ege, Fac Sci, Dept Chem, TR-35100 Izmir, Turkey; [Sahin, Zarife Sibel] Univ Sinop, Sci & Technol Res Applicat & Res Ctr, Sinop, Turkey in 2020, Cited 44. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A series of monometallic complexes (Ru1-3, Ir-1(-3)) which have N,O-chelating ligand (pyrazine-2carboxylate (1), pyridine-2-carboxylate (2), quinoline carboxylate(3) and bimetallic complexes (Ru-4,Ru-5, Ir-4(,5)) bridged by pyrazine-2,3- dicarboxylate (4) and imidazole-4,5-dicarboxylate(5) were synthesized and characterized by H-1-, C-13 NMR, FT-IR, and elemental analysis. The crystal structure of Ir-2 was determined by X-ray crystallography. The complexes (Ru1-5, Ir1-5) were applied to investigate the electronic and steric effect of ligand in their catalytic activities in transfer hydrogenation and alpha(alpha)-alkylation reaction of ketones with alcohols. The activities of iridium complexes (Ir1-5) were much more efficient than ruthenium complexes (Ru1-5). The highest activity for both reactions was observed for the complex (Ir2 ) with pyridine-2-carboxylate. The Ir hydride species was monitored for both reactions. (C) 2020 Elsevier B.V. All rights reserved.

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

Authors Ragunathan, P; Cole, M; Latka, C; Aragaw, WW; Hegde, P; Shin, J; Manimekalai, MSS; Rishikesan, S; Aldrich, CC; Dick, T; Gruber, G in AMER CHEMICAL SOC published article about ASPARTATE-ALPHA-DECARBOXYLASE; PYRAZINAMIDE RESISTANCE; CRYSTAL-STRUCTURE; ATP SYNTHESIS; MUTATIONS; EXPRESSION; SYNTHASE in [Ragunathan, Priya; Latka, Chitra; Shin, Joon; Manimekalai, Malathy Sony Subramanian; Rishikesan, Sankaranarayanan; Gruber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore 637551, Singapore; [Cole, Malcolm; Hegde, Pooja; Aldrich, Courtney C.] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA; [Aragaw, Wassihun Wedajo; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Dick, Thomas] Hackensack Meridian Sch Med, Dept Med Sci, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20007 USA in 2021, Cited 28. Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A common strategy employed in antibacterial drug discovery is the targeting of biosynthetic processes that are essential and specific for the pathogen. Specificity in particular avoids undesirable interactions with potential enzymatic counterparts in the human host, and it ensures ontarget toxicity. Synthesis of pantothenate (Vitamine B5), which is a precursor of the acyl carrier coenzyme A, is an example of such a pathway. In Mycobacterium tuberculosis (Mtb), which is the causative agent of tuberculosis (TB), pantothenate is formed by pantothenate synthase, utilizing D-pantoate and beta-Ala as substrates. beta-Ala is mainly formed by the decarboxylation of L-aspartate, generated by the decarboxylase PanD, which is a homo-oliogomer in solution. Pyrazinoic acid (POA), which is the bioactive form of the TB prodrug pyrazinamide, binds and inhibits PanD activity weakly. Here, we generated a library of recombinant Mtb PanD mutants based on structural information and PZA/POA resistance mutants. Alterations in oligomer formation, enzyme activity, and/or POA binding were observed in respective mutants, providing insights into essential amino acids for Mtb PanD’s proper structural assembly, decarboxylation activity and drug interaction. This information provided the platform for the design of novel POA analogues with modifications at position 3 of the pyrazine ring. Analogue 2, which incorporates a bulky naphthamido group at this position, displayed a 1000-fold increase in enzyme inhibition, compared to POA, along with moderately improved antimycobacterial activity. The data demonstrate that an improved understanding of mechanistic and enzymatic features of key metabolic enzymes can stimulate design of more-potent PanD inhibitors.

Welcome to talk about 98-97-5, If you have any questions, you can contact Ragunathan, P; Cole, M; Latka, C; Aragaw, WW; Hegde, P; Shin, J; Manimekalai, MSS; Rishikesan, S; Aldrich, CC; Dick, T; Gruber, G or send Email.. Formula: C5H4N2O2

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

Authors Packiaraj, S; Kousalya, L; Pushpaveni, A; Poornima, S; Puschmann, H; Govindarajan, S in SPRINGER published article about in [Packiaraj, S.] Sri Krishna Coll Engn & Technol, Sci & Humanities Chem, Coimbatore 641008, Tamil Nadu, India; [Packiaraj, S.; Pushpaveni, A.; Poornima, S.; Govindarajan, S.] Bharathiar Univ, Dept Chem, Coimbatore 641046, Tamil Nadu, India; [Kousalya, L.] Nirmala Coll Women, Dept Bot, Coimbatore 641018, Tamil Nadu, India; [Pushpaveni, A.] Kongunadu Arts & Sci Coll, Dept Chem, Coimbatore 641029, Tamil Nadu, India; [Puschmann, H.] Univ Durham, Dept Chem, South Rd, Durham DH1 3LE, England in 2021, Cited 43. SDS of cas: 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

In general, molecules with certain functional groups such as amine (-NH2) and carboxyl (-COOH) can promote the growth of co-crystals leading to the formation of supramolecular networks. However, if the differences in the pKa values of the two molecules are large [pKa (base)-pKa (acid)], salts can result instead of ‘real’ co-crystals. Here, we report the formation of such salt by letting pyrazine-2-carboxylic acid (pKa = 2.9) crystallize together with aminoguanidine (pKa = 11.5; high Delta pka = 8.6) a nitrogen-rich organic base. The title salt has been prepared by slow evaporation of an equimolar ratio of guanylhydrazine bicarbonate (i.e., aminoguanidine bicarbonate (AgunH.HCO3)) and pyrazine-2-carboxylic acid (Pymca) in aqueous medium. The salt was characterized by IR spectroscopy, powder and single-crystal X-ray diffraction techniques. This material shows enhanced antioxidant activity and this is due to the crucial role of hydrazinic moiety in the aminoguanidinium salt.

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

Florentini, EA; Angulo, N; Gilman, RH; Alcantara, R; Roncal, E; Antiparra, R; Toscano, E; Vallejos, K; Kirwan, D; Zimic, M; Sheen, P in [Florentini, Edgar A.; Angulo, Noelia; Alcantara, Roberto; Roncal, Elisa; Antiparra, Ricardo; Toscano, Emily; Vallejos, Katherine; Kirwan, Danni; Zimic, Mirko; Sheen, Patricia] Univ Peruana Cayetano Heredia, Fac Ciencias & Filosofia, Lab Invest & Desarrollo, Lab Bioinformat & Biol Mol, Lima, Peru; [Gilman, Robert H.] Johns Hopkins Bloomberg Sch Publ Hlth, Dept Int Hlth, Baltimore, MD USA published Immunological detection of pyrazine-2-carboxylic acid for the detection of pyrazinamide resistance in Mycobacterium tuberculosis in 2020, Cited 28. 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.

Pyrazinamide (PZA) susceptibility testing in Mycobacterium tuberculosis (Mtb) is a current area of development and PZA-resistant strains are increasingly prevalent. Previous studies have demonstrated that the detection of pyrazinoic acid (POA), the metabolite produced by the deamidation of PZA, is a good predictor for PZA resistance since a resistant strain would not convert PZA into POA at a critical required rate, whereas a susceptible strain will do, expelling POA to the extracellular environment at a certain rate, and allowing for quantification of this accumulated analyte. In order to quantify POA, an indirect competitive ELISA (icELISA) test using hyperimmune polyclonal rabbit serum against POA was developed: for this purpose, pure POA was first covalently linked to the highly immunogenic Keyhole Limpet Hemocyanine, and inoculated in rabbits. A construct made of bovine serum albumin (BSA) linked to pure POA and fixed at the bottom of wells was used as a competitor against spiked samples and liquid Mtb culture supernatants. When spiked samples (commercial POA alone) were analyzed, the half maximal inhibitory concentration (IC50) was 1.16 mg/mL, the limit of detection 200 mu g/mL and the assay was specific (it did not detect PZA, IC50 > 20 mg/mL). However, culture supernatants (7H9-OADC-PANTA medium) disrupted the competition and a proper icELISA curve was not obtainable. We consider that, although we have shown that it is feasible to induce antibodies against POA, matrix effects could damage its analytical usefulness; multiple, upcoming ways to solve this obstacle are suggested.

Welcome to talk about 98-97-5, If you have any questions, you can contact Florentini, EA; Angulo, N; Gilman, RH; Alcantara, R; Roncal, E; Antiparra, R; Toscano, E; Vallejos, K; Kirwan, D; Zimic, M; Sheen, P or send Email.. Safety of Pyrazine-2-carboxylic acid

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

Formula: C5H4N2O2. 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.

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

Authors Mugabo, P; Mulubwa, M in SPRINGER FRANCE 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. HPLC of 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.

HPLC of Formula: 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

An article Evaluation and Docking Study of Pyrazine Containing 1, 3, 4-Oxadiazoles Clubbed with Substituted Azetidin-2-one: A New Class of Potential Antimicrobial and Antitubercular WOS:000575832100001 published article about MYCOBACTERIUM-TUBERCULOSIS; ANTIINFLAMMATORY ACTIVITY; LUMAZINE SYNTHASE; BINDING MODE; BETA-LACTAMS; 1,3,4-OXADIAZOLE; AZETIDINONES; RESISTANCE; INHIBITORS; DESIGN in [Das, Rina; Mehta, Dinesh Kumar] Maharishi Markandeshwar Deemed Be Univ, MM Coll Pharm, Ambala 133207, Haryana, India in 2021, Cited 50. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Category: Pyrazines

Background Tuberculosis (TB) caused by Mycobacterium tuberculosis is one of the main killers of people all over the world. The major hurdles with existing therapy are the lengthy regimen and appearance of multi drug resistant (MDR) and extensively drug resistant (XDR) strains of M.tuberculosis. Aims The present work was aimed to synthesize and determine antitubercular and antimicrobial potential of some novel 3-chloro-4-aryl-1-[4-(5-pyrazin-2-yl[1,3,4]oxadiazole-2-ylmethoxy)-phenyl]-azetidin-2-one derivatives 7(a-h) from pyrazinoic acid as precursor, which is a well-established antitubercular agent. Here we report the synthesis of a new class of heterocyclic molecules in which pyrazine, 1, 3, 4-oxadiazole and azetidinone moieties were present in one frame work. Methods Pyrazinoic acid (1) was esterified first (2) followed by amination to produce hydrazide (3) which was refluxed with POCl3 to obtain 2-chloromethyl-5pyrazino-1, 3, 4-oxadiazole (4). This was then further reacted with 4-amino phenol to obtain 4-[5-pyrazino-1, 3, 4-oxadiazol-2-yl-methoxy]-phenyl amine (5) which on condensation with various aromatic aldehydes afforded a series Schiff’s bases 6(a-h). Dehydrative annulations of 6(a-h) in the presence of chloroacetyl chloride and triethylamine yielded 3-chloro-4-aryl-1-[4-(5-pyrazin-2-yl-[1, 3, 4]oxadiazole-2-ylmethoxy)-phenyl]-azetidin-2-one derivatives 7(a-h). Antibacterial, antifungal and antitubercular potential of all the synthesized compounds were assessed. Docking study was performed using the software VLife Engine tools of Vlifemds 4.6 on the protein lumazine synthase of M. tuberculosis (PDB entry code 2C92). Results The present studies demonstrated that synthesized oxadiazole derivatives have good antimicrobial activity against the various microorganisms. Among the synthesized derivative, 7b and 7g were found to be prominent compounds which have potential antibacterial, antifungal and antitubercular activity (with MIC 3.12 mu g/ml and high dock score ranging from -59.0 to -54.0) against Mycobacterium tuberculosis. Conclusions Derivatives 7b and 7g would be effective lead candidates for tuberculosis therapy.

Category: Pyrazines. 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 2021 EUR J ORG CHEM published article about ONE-POT SYNTHESIS; MULTICOMPONENT REACTIONS; POSTCONDENSATION MODIFICATIONS; BUILDING-BLOCKS; SOLID-STATE; ISOCYANIDE; HEXAMETHYLENETETRAMINE; CHEMISTRY; AMMONIA; MECHANISM in [Rosalba, Thaissa Pasquali F.; Kas, Samia Sayegh A.; Sampaio, Ana Beatriz S.; Salvador, Carlos Eduardo M.; Andrade, Carlos Kleber Z.] Univ Brasilia, Inst Quim, Lab Quim Metodol & Organ Sintet LaQMOS, Campus Univ, BR-70904970 Brasilia, DF, Brazil in 2021, Cited 98. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: Pyrazine-2-carboxylic acid

Ugi reactions are still a challenge when the concomitant use of ammonia and formaldehyde is required. Herein, we propose a strategy to overcome this challenge using hexamethylenetetramine (HMTA) as a singular key for the employment of these two simple starting materials in the Ugi reaction. Acylaminoacetamide derivatives were prepared in good to excellent yields by this new methodology. The scope and optimization of the reaction conditions were investigated. This novel methodology was successfully applied in the synthesis of two different diketopiperazines (DKPs) using the Ugi/Deprotection+Activation/Cyclization (UDAC) method. A continuous flow approach was also used in this methodology.

Welcome to talk about 98-97-5, If you have any questions, you can contact Rosalba, TPF; Kas, SSA; Sampaio, ABS; Salvador, CEM; Andrade, CKZ or send Email.. Recommanded Product: Pyrazine-2-carboxylic acid

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

In 2020 J BIOL INORG CHEM published article about MYCOBACTERIUM-TUBERCULOSIS; PRUSSIAN BLUE; NITROXYL; PYRAZINAMIDE; INSIGHTS; DRUG; ACTIVATION; MECHANISMS; RESISTANCE; NO in [Carvalho, Edinilton Muniz; Paulo, Tercio de Freitas; Saquet, Alix Sournia; Chauvin, Remi; Bernardes-Genisson, Vania] CNRS, Lab Chim Coordinat, LCC, UPR 8241, 205 Route Narbonne,BP 44099, F-31077 Toulouse 4, France; [Carvalho, Edinilton Muniz; Paulo, Tercio de Freitas; Chauvin, Remi; Bernardes-Genisson, Vania] Univ Toulouse, Univ Paul Sabatier, UPS, 118 Route Narbonne, F-31062 Toulouse 9, France; [Carvalho, Edinilton Muniz; Paulo, Tercio de Freitas; Franca Lopes, Luiz Gonzaga; Silva Sousa, Eduardo Henrique] Univ Fed Ceara, Dept Quim Organ & Inorgan, Grp Bioinorgen, Campus Pici, BR-60455760 Fortaleza, Ceara, Brazil; [Abbadi, Bruno Lopes; Macchi, Fernanda Souza; Bizarro, Cristiano Valim] Pontificia Univ Catolica Rio Grande Do Sul PUCRS, Ctr Pesquisas Biol Mol & Func CPBMF, Porto Alegre, RS, Brazil; [Abbadi, Bruno Lopes; Macchi, Fernanda Souza; Bizarro, Cristiano Valim; Franca Lopes, Luiz Gonzaga; Silva Sousa, Eduardo Henrique] Inst Nacl Ciencia & Tecnol TB INCT TB, Porto Alegre, RS, Brazil; [Campos, Rafael de Morais; Abrantes Ferreira, Talles Luann; Falcao do Nascimento, Nilberto Robson] Univ Estadual Ceara, Lab Farmacol Cardiovasc & Renal, Campus Itaperi, BR-60714903 Fortaleza, Ceara, Brazil in 2020, Cited 40. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. COA of Formula: C5H4N2O2

A pharmacophore design approach, based on the coordination chemistry of an intimate molecular hybrid of active metabolites of pro-drugs, known to release active species upon enzymatic oxidative activation, is devised. This is exemplified by combining two anti-mycobacterial drugs: pyrazinamide (first line) and delamanid (third line) whose active metabolites are pyrazinoic acid (PyzCOOH) and likely nitroxyl (HNO (or NO.)), respectively. Aiming to generate those active species, a hybrid compound was envisaged by coordination of pyrazine-2-hydroxamic acid (PyzCONHOH) with a Na-3[Fe-II(CN)(5)] moiety. The corresponding pentacyanoferrate(II) complex Na-4[Fe-II(CN)(5)(PyzCONHO(-))] was synthesized and characterized by several spectroscopic techniques, cyclic voltammetry, and DFT calculations. Chemical oxidation of this complex with H(2)O(2)was shown to induce the release of the metabolite PyzCOOH, without the need of theMycobacterium tuberculosis(Mtb) pyrazinamidase enzyme (PncA). Control experiments show that both H2O2- and N-coordinated pyrazine Fe(II)species are required, ruling out a direct hydrolysis of the hydroxamic acid or an alternative oxidative route through chelation of a metal center by a hydroxamic group. The release of HNO was observed using EPR spectroscopy in the presence of a spin trapping agent. The devised iron metal complex of pyrazine-2-hydroxamic acid was found inactive against an actively growing/non-resistantMtbstrain; however, it showed a strong dose-dependent and reversible vasodilatory activity with mostly lesser toxic effects than the reference drug sodium nitroprussiate, unveiling thus a potential indication for acute or chronic cardiovascular pathology. This is a priori a further indirect evidence of HNO release from this metal complex, standing as a possible pharmacophore model for an alternative vasodilator drug.

COA of Formula: C5H4N2O2. 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 2021 ACS CHEM BIOL published article about ASPARTATE-ALPHA-DECARBOXYLASE; PYRAZINAMIDE RESISTANCE; CRYSTAL-STRUCTURE; ATP SYNTHESIS; MUTATIONS; EXPRESSION; SYNTHASE in [Ragunathan, Priya; Latka, Chitra; Shin, Joon; Manimekalai, Malathy Sony Subramanian; Rishikesan, Sankaranarayanan; Gruber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore 637551, Singapore; [Cole, Malcolm; Hegde, Pooja; Aldrich, Courtney C.] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA; [Aragaw, Wassihun Wedajo; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Dick, Thomas] Hackensack Meridian Sch Med, Dept Med Sci, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20007 USA in 2021, Cited 28. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Quality Control of Pyrazine-2-carboxylic acid

A common strategy employed in antibacterial drug discovery is the targeting of biosynthetic processes that are essential and specific for the pathogen. Specificity in particular avoids undesirable interactions with potential enzymatic counterparts in the human host, and it ensures ontarget toxicity. Synthesis of pantothenate (Vitamine B5), which is a precursor of the acyl carrier coenzyme A, is an example of such a pathway. In Mycobacterium tuberculosis (Mtb), which is the causative agent of tuberculosis (TB), pantothenate is formed by pantothenate synthase, utilizing D-pantoate and beta-Ala as substrates. beta-Ala is mainly formed by the decarboxylation of L-aspartate, generated by the decarboxylase PanD, which is a homo-oliogomer in solution. Pyrazinoic acid (POA), which is the bioactive form of the TB prodrug pyrazinamide, binds and inhibits PanD activity weakly. Here, we generated a library of recombinant Mtb PanD mutants based on structural information and PZA/POA resistance mutants. Alterations in oligomer formation, enzyme activity, and/or POA binding were observed in respective mutants, providing insights into essential amino acids for Mtb PanD’s proper structural assembly, decarboxylation activity and drug interaction. This information provided the platform for the design of novel POA analogues with modifications at position 3 of the pyrazine ring. Analogue 2, which incorporates a bulky naphthamido group at this position, displayed a 1000-fold increase in enzyme inhibition, compared to POA, along with moderately improved antimycobacterial activity. The data demonstrate that an improved understanding of mechanistic and enzymatic features of key metabolic enzymes can stimulate design of more-potent PanD inhibitors.

Quality Control of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Ragunathan, P; Cole, M; Latka, C; Aragaw, WW; Hegde, P; Shin, J; Manimekalai, MSS; Rishikesan, S; Aldrich, CC; Dick, T; Gruber, G or send Email.

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