Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: Anti-Mycobacterium tuberculosis activity and cytotoxicity
Contribuinte(s) |
UNIVERSIDADE DE SÃO PAULO |
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Data(s) |
20/10/2012
20/10/2012
2010
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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 |
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 |