Journal
ARCHIV DER PHARMAZIE
Volume 344, Issue 3, Pages 178-183Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201000013
Keywords
Antibacterial activity; Helicobacter pylori; 5-Nitroimidazole; 1,3,4-Thiadiazole
Funding
- Tehran University of Medical Sciences, Tehran, Iran
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A series of 5-nitroimidazole-based 1,3,4-thiadiazoles were prepared and tested for antibacterial activity against Helicobacter pylori. The anti-H. pylori activity of target compounds along with the commercially available antimicrobial metronidazole was evaluated by comparing the inhibition-zone diameters determined by the paper disc diffusion bioassay. From our bioassay results against 20 clinical isolates it is evident that piperazinyl, 4-methylpiperazinyl, 3-methylpiperazinyl, and 3,5-dimethylpiperazinyl analogs (6a, 6b, 6e, and 6f, respectively) and pyrrolidine derivative 7 had strong activity at 0.5 mu g/disc (average of inhibition zone >20 mm) while metronidazole had no activity at this dose. Compound 6f containing the 3,5-dimethylpiperazinyl moiety at the 2-position of the 5-(1-methyl-5-nitro-1H-imidazol-2-yl)-1,3,4-thiadiazole skeleton was the most potent compound tested at low concentrations.
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