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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
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]
Total Authors: 8
Affiliation:
[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
Total Affiliations: 6
Document type: Journal article
Source: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 45, n. 5, p. 1898-1905, MAY 2010.
Web of Science Citations: 164
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, 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)

FAPESP's process: 08/10390-2 - Determination of pre-clinical profile in vitro and in vivo anti-tuberculosis activity of ruthenium(II)phosphine / picolinate complexes
Grantee:Fernando Rogério Pavan
Support Opportunities: Scholarships in Brazil - Doctorate