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

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

Volume: 6 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Foroumadi Alireza, Sedaghat Somayeh, Emami Saeed, Yazdanian Maryam, Moshafi Hassan Mohammad, Safavi Maliheh, Sakhteman Amirhossein, Firoozpour Loghman, Vosooghi Mohsen and Shafiee Abbas, Synthesis and Structure-Activity Relationship Study of 2-Substituted- 5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles as Anti-Helicobacter pylori Agents, Letters in Drug Design & Discovery 2009; 6 (6) . https://dx.doi.org/10.2174/157018009789057599