4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 5, Pages 1898-1905

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.01.028

Keywords

Antimycobacterial agents; REMA; Cytotoxicity; Thiosemicarbazones; Semicarbazones; Dithiocarbazates; Hydrazide/hydrazones

Funding

  1. CNPq
  2. Capes
  3. Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2008/10390-2, 2009/06499-1]

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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 (IC50) was determined to establish a selectivity index (SI) (SI = IC50/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.

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