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


Autoria(s): PAVAN, Fernando R.; MAIA, Pedro I. da S.; LEITE, Sergio R. A.; DEFLON, Victor M.; BATISTA, Alzir A.; SATO, Daisy N.; FRANZBLAU, Scott G.; LEITE, Clarice Q. F.
Contribuinte(s)

UNIVERSIDADE DE SÃO PAULO

Data(s)

20/10/2012

20/10/2012

2010

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.

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

CNPq

Capes

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)[2008/10390-2]

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)[2009/06499-1]

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Identificador

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.45, n.5, p.1898-1905, 2010

0223-5234

http://producao.usp.br/handle/BDPI/31809

10.1016/j.ejmech.2010.01.028

http://dx.doi.org/10.1016/j.ejmech.2010.01.028

Idioma(s)

eng

Publicador

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

Relação

European Journal of Medicinal Chemistry

Direitos

restrictedAccess

Copyright ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

Palavras-Chave #Antimycobacterial agents #REMA #Cytotoxicity #Thiosemicarbazones #Semicarbazones #Dithiocarbazates #Hydrazide/hydrazones #IN-VITRO #ISONICOTINOYL HYDRAZONE #ANTITUMOR-ACTIVITY #CRYSTAL-STRUCTURE #IRON CHELATORS #2-ACETYLPYRIDINE THIOSEMICARBAZONES #ANTIMYCOBACTERIAL ACTIVITY #ANTIPROLIFERATIVE AGENTS #BENZOYL HYDRAZONE #REDOX ACTIVITY #Chemistry, Medicinal
Tipo

article

original article

publishedVersion