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

Author(s): Alireza Foroumadi, Somayeh Sedaghat, Saeed Emami, Maryam Yazdanian, Mohammad Hassan Moshafi, Maliheh Safavi, Amirhossein Sakhteman, Loghman Firoozpour, Mohsen Vosooghi, Abbas Shafiee.

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 6 , 2009

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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.

Keywords: Antibacterial activity, Anti-Helicobacter pylori activity, 1,3,4-Thiadiazole, Nitrothiophene

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Article Details

VOLUME: 6
ISSUE: 6
Year: 2009
Page: [468 - 474]
Pages: 7
DOI: 10.2174/157018009789057599
Price: $58

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