Synthesis and evaluation of a pyrazinoic acid prodrug in Mycobacterium tuberculosis
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Data
2014-09-01
Autores
Fernandes, Joao Paulo-dos Santos
Pavan, Fernando Rogério [UNESP]
Leite, Clarice Queico Fujimura [UNESP]
Andres Felli, Veni Maria
Título da Revista
ISSN da Revista
Título de Volume
Editor
Elsevier B.V.
Resumo
Tuberculosis (TB) is a disease caused mainly by infection of Mycobacterium tuberculosis affecting more than ten million people around the world. Despite TB can be treated, the rise of MDR-TB and XDR-TB cases put the disease in a worrying status. As pyrazinamide-resistant strains exhibit low or none pyrazinamidase activity, it is proposed that the active form of pyrazinamide (PZA) is pyrazinoic acid (POA), although this acid has poor penetration in mycobacteria. In this work, we present a convenient one-pot synthesis of 2-chloroethyl pyrazinoate, and its activity in M. tuberculosis H(37)Rv (ATCC27294) in MIC assay using the MABA technique. The obtained MIC of the compound was 3.96 g/mL, and discussion about the activity profile of some previously evaluated pyrazinoates is also performed. (C) 2013 King Saud University. Production and hosting by Elsevier B.V. All rights reserved.
Descrição
Palavras-chave
Antimycobacterial agent, Ester synthesis, Prodrug, Pyrazinoic acid, Tuberculostatic
Como citar
Saudi Pharmaceutical Journal. Amsterdam: Elsevier Science Bv, v. 22, n. 4, p. 376-380, 2014.