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