Artigo
Synthesis and evaluation of a pyrazinoic acid prodrug in Mycobacterium tuberculosis
Registro en:
Saudi Pharmaceutical Journal. Amsterdam: Elsevier Science Bv, v. 22, n. 4, p. 376-380, 2014.
1319-0164
10.1016/j.jsps.2013.12.005
WOS:000341120900013
WOS000341120900013.pdf
2114570774349859
Autor
Fernandes, Joao Paulo-dos Santos
Pavan, Fernando Rogério [UNESP]
Leite, Clarice Queico Fujimura [UNESP]
Andres Felli, Veni Maria
Resumen
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. Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) PROPE Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Fed Univ Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Sao Paulo, Brazil State Univ Sao Paulo UNESP, Fac Pharmaceut Sci, Dept Biol Sci, Sao Paulo, Brazil Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, BR-05508 Sao Paulo, Brazil State Univ Sao Paulo UNESP, Fac Pharmaceut Sci, Dept Biol Sci, Sao Paulo, Brazil