Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: anti-Mycobacterium tuberculosis activity and cytotoxicity.

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作者：

FR Pavan，PIDS Maia，SRA Leite，VM Deflon，AA Batista，DN Sato，SG Franzblau，CQF Leite

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摘要：

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, dithiocarbazates 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.

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关键词：

Antimycobacterial agents REMA Cytotoxicity Thiosemicarbazones Semicarbazones Dithiocarbazates Hydrazide/hydrazones

DOI：

10.1016/j.ejmech.2010.01.028

被引量：

254

年份：

2010