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

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 comp...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2010-05, Vol.45 (5), p.1898-1905
Main Authors: 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.
Format: Article
Language:English
Subjects:
Animals
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimycobacterial agents
Antitubercular Agents - chemical synthesis
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Biological and medical sciences
Cell Line
Cell Survival - drug effects
Crystallography, X-Ray
Cytotoxicity
Dithiocarbazates
Hydrazide/hydrazones
Hydrazines - chemical synthesis
Hydrazines - chemistry
Hydrazines - pharmacology
Medical sciences
Mice
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Mycobacterium tuberculosis - drug effects
Mycobacterium tuberculosis - metabolism
Pharmacology. Drug treatments
REMA
Semicarbazones
Semicarbazones - chemical synthesis
Semicarbazones - chemistry
Semicarbazones - pharmacology
Structure-Activity Relationship
Thiosemicarbazones
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Summary: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 (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. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2010.01.028