The Synthesis, Structure and Activity Evaluation of Secnidazole Derivatives as Helicobacter pylori Urease Inhibitors

Author(s): Xi-Shou Huang, Kai Liu, Yong Yin, Wan-Mei Li, Wei Ran, Man Duan, Li-Sheng Wang, Hai-Liang Zhu.

Journal Name:Current Bioactive Compounds

Volume 7 , Issue 4 , 2011

Abstract:

Thirty secnidazole derivatives have been synthesized and evaluated for Helicobacter pylori (H. Pylori) urease inhibitory activities and anti-inflammatory activities. All of them were reported for the first time. Their chemical structures were characterized by 1H NMR, 13C NMR, MS, and elemental analysis. Compound 5a, 6c and 8c showed the most potent urease inhibitory activities and anti-inflammatory activities with IC50 values of 1.7 μM, 1.0 μM, 2.0 μM and inhibition of 62.60%, 59.54%, 71.76%, respectively. Docking simulation was performed to position compound 6c into the urease active site to determine the probable binding model. Compound 5a, 6c and 8c with potent inhibitory activity against H. pylori may be potential antibacterial agents.

Keywords: Urease inhibitors, Helicobacter pylori, secnidazole derivatives, salicyclic acid derivatives, anti-inflammatory activites, docking, antibacterial agent, urea hydrolase, gastroduodenal diseases, living organisms

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Article Details

VOLUME: 7
ISSUE: 4
Year: 2011
Page: [268 - 280]
Pages: 13
DOI: 10.2174/157340711798375868
Price: $58