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
Letters in Drug Design & Discovery
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.
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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
DOI https://dx.doi.org/10.2174/157018009789057599 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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