Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: Anti-Mycobacterium tuberculosis activity and cytotoxicity
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Data
2010-05-01
Autores
Pavan, Fernando Rogério [UNESP]
Maia, Pedro I. da S.
Leite, Sergio R. A. [UNESP]
Deflon, Victor M.
Batista, Alzir A.
Sato, Daisy N.
Franzblau, Scott G.
Leite, Clarice Queico Fujimura [UNESP]
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Elsevier France-editions Scientifiques Medicales Elsevier
Resumo
The aim of this study was to identify a candidate drug for the development of anti-tuberculosis therapy from previously synthesized compounds based on the thiosemicarbazones, semicarbazones, dithio-carbazates and hydrazide/hydrazones compounds. The minimal inhibitory concentration (MIC) of these compounds against Mycobacterium tuberculosis was determined. Their in vitro cytotoxicity to J774 cells (IC(50)) was determined to establish a selectivity index (SI) (SI = IC(50)/MIC). The best compounds were the thiosemicarbazones (2, 3 and 4) and the hydrazide/hydrazones (14, 15, 16 and 18). The results are comparable to or better than those of "first line" or "second line" drugs commonly used to treat TB, suggesting these compounds as anti-TB drug candidates. (C) 2010 Elsevier Masson SAS. All rights reserved.
Descrição
Palavras-chave
Antimycobacterial agents, REMA, Cytotoxicity, Thiosemicarbazones, Semicarbazones, Dithiocarbazates, Hydrazide/hydrazones
Como citar
European Journal of Medicinal Chemistry. Paris: Elsevier France-editions Scientifiques Medicales Elsevier, v. 45, n. 5, p. 1898-1905, 2010.