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 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.
Klimesová
Vera
V
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic. klimeso@faf.cuni.cz
Kocí
Jan
J
Waisser
Karel
K
Kaustová
Jarmila
J
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D001562:Benzimidazoles