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

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

  • Eur J Med Chem. 2010 May;45(5):1898-905. doi: 10.1016/j.ejmech.2010.01.028.
Fernando R Pavan 1,  Pedro I da S Maia,  Sergio R A Leite,  Victor M Deflon,  Alzir A Batista,  Daisy N Sato,  Scott G Franzblau,  Clarice Q F Leite
Affiliations

Affiliation

  • 1 Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, 14801-902 Araraquara, SP, Brazil. pavanfer@yahoo.com.br
PMID: 20163897 DOI: 10.1016/j.ejmech.2010.01.028
Abstract

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 (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.

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