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

Autor(es)

Pavan, Fernando R. ^[1] ; Maia, Pedro I. da S. ^[2] ; Leite, Sergio R. A. ^[3] ; Deflon, Victor M. ^[2] ; Batista, Alzir A. ^[4] ; Sato, Daisy N. ^[5] ; Franzblau, Scott G. ^[6] ; Leite, Clarice Q. F. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil

^[2] Univ Sao Paulo, Inst Quim Sao Carlos, BR-1356659 Sao Carlos, SP - Brazil

^[3] Univ Estadual Paulista, Inst Quim, BR-14800900 Araraquara, SP - Brazil

^[4] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil

^[5] Inst Adolfo Lutz Registro, Unidade Ribeirao Preto, BR-14085410 Ribeirao Preto, SP - Brazil

^[6] Univ Illinois, Coll Pharm, Inst TB Res, Chicago, IL - USA

• Tipo de documento: Artigo Científico
• Fonte: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 45, n. 5, p. 1898-1905, MAY 2010.
• Citações Web of Science: 164

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. (AU)

• Processo FAPESP: 08/10390-2 - Determinação do perfil pré-clínico da atividade antituberculose in vitro e in vivo dos complexos de rutênio(II)fosfinas / diiminas
• Beneficiário: Fernando Rogério Pavan
• Modalidade de apoio: Bolsas no Brasil - Doutorado