title: Thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones: anti-Mycobacterium tuberculosis activity and cytotoxicity.
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.
authors.affiliation: Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, 14801-902 Araraquara, SP, Brazil. pavanfer@yahoo.com.br
authors.forename: Fernando R
authors.initials: FR
authors.lastname: Pavan
authors.forename: Pedro I
authors.initials: PI
authors.lastname: da S Maia
authors.forename: Sergio R A
authors.initials: SR
authors.lastname: Leite
authors.forename: Victor M
authors.initials: VM
authors.lastname: Deflon
authors.forename: Alzir A
authors.initials: AA
authors.lastname: Batista
authors.forename: Daisy N
authors.initials: DN
authors.lastname: Sato
authors.forename: Scott G
authors.initials: SG
authors.lastname: Franzblau
authors.forename: Clarice Q F
authors.initials: CQ
authors.lastname: Leite
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000378:metabolism; D012664:Semicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000995:Antitubercular Agents; D006834:Hydrazines; D012664:Semicarbazones