Home >> Letters in Drug Design & Discovery, Volume 6, Number 6

Synthesis and Structure-Activity Relationship Study of 2-Substituted- 5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles as Anti-Helicobacter pylori Agents

Authors: Foroumadi, Alireza; Sedaghat, Somayeh; Emami, Saeed; Yazdanian, Maryam; Moshafi, Mohammad H.; Safavi, Maliheh; Sakhteman, Amirhossein; Firoozpour, Loghman; Vosooghi, Mohsen; Shafiee, Abbas

Source: Letters in Drug Design & Discovery, Volume 6, Number 6, September 2009 , pp. 468-474(7)

Publisher: Bentham Science Publishers

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Abstract:

Some alkylthio, alkylsulfinyl and alkylsulfonyl-5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles were synthesized and evaluated against Helicobacter pylori. The antibacterial data indicated that most compounds exhibited significant inhibitory activity against H. pylori- more potent than standard drug metronidazole. Among them, 2-ethylsulfinyl-5-(5-nitro-2- thienyl)-1,3,4-thiadiazole was the most potent compound tested against clinical isolates of H. pylori. Generally the SAR of this series of compounds indicated that both the structure of the alkyl pendent and the S, SO or SO2 linker dramatically impact the antibacterial activity against H. pylori.

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
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