New benzimidazole derivatives as antimycobacterial agents

A set of 2-alkylsulfanyl derivatives of 5-methylbenzimidazole was synthesized and evaluated for antimycobacterial activity. The structures of the compounds were confirmed by 1H NMR and IR data, and their purity by elemental analysis. Antimycobacterial activities against Mycobacterium tuberculosis an...

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Bibliographic Details
Published in:Farmaco (Società chimica italiana : 1989) 2002-04, Vol.57 (4), p.259-265
Main Authors: Klimešová, Věra, Kočı́, Jan, Waisser, Karel, Kaustová, Jarmila
Format: Article
Language:English
Subjects:
2-Alkylsulfanyl derivatives
5-Methylbenzimidazole-2-thiol
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimycobacterial activity
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Magnetic Resonance Spectroscopy
Medical sciences
Microbial Sensitivity Tests
Mycobacterium - drug effects
Mycobacterium tuberculosis
Nontuberculous mycobacteria
Pharmacology. Drug treatments
Spectrophotometry, Infrared
Structure-Activity Relationship
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Summary:A set of 2-alkylsulfanyl derivatives of 5-methylbenzimidazole was synthesized and evaluated for antimycobacterial activity. The structures of the compounds were confirmed by 1H NMR and IR data, and their purity by elemental analysis. Antimycobacterial activities against Mycobacterium tuberculosis and nontuberculous mycobacteria were expressed as the minimum inhibitory concentration. The substances exhibited significant antimycobacterial activity, in particular against both strains of Mycobacterium kansasii. The effect of the most active compound in the set, 3,5-dinitro derivative 3t, exceeded that of the standard isoniazide against M. kansasii and Mycobacterium avium.
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(02)01218-1