5‐Nitroimidazole‐based 1,3,4‐Thiadiazoles: Heterocyclic Analogs of Metronidazole as Anti‐ Helicobacter pylori Agents
2010; Wiley; Volume: 344; Issue: 3 Linguagem: Inglês
10.1002/ardp.201000013
ISSN1521-4184
AutoresMohammad Hassan Moshafi, Maedeh Sorkhi, Saeed Emami, Maryam Nakhjiri, Azadeh Yahya‐Meymandi, Amirsoheil Negahbani, Farideh Siavoshi, Maryam Omrani, Eskandar Alipour, Mohsen Vosooghi, Abbas Shafiee, Alireza Foroumadi,
Tópico(s)Clostridium difficile and Clostridium perfringens research
ResumoAbstract 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 µg/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‐1 H ‐imidazol‐2‐yl)‐1,3,4‐thiadiazole skeleton was the most potent compound tested at low concentrations.
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