ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)
Volume 13, 10 Issues, 2016
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Design, Synthesis and Biological Evaluation of Some Oxadiazole Derivatives as Novel Amide-Based Inhibitors of Soluble Epoxide Hydrolase
Letters in Drug Design & Discovery, 11
): 721-730.Author(s): Elham Rezaee Zavareh
, Mahdi Hedayati
, Laleh Hoghooghi Rad
, Azin Kiani
, Soraya Shahhosseini
, Mehrdad Faizi
and Sayyed Abbas Tabatabai
Department of Pharmaceutical Chemistry, School of Pharmacy, Pytochemistry Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
AbstractSoluble epoxide hydrolase (sEH) enzyme plays an important role in the metabolism of endogenous chemical mediators which are involved in the regulation of blood pressure and inflammation. Although the most reported potent sEH inhibitors are urea derivatives, these compounds have limited pharmacokinetic profile. In order to improve physicochemical properties, besides having favorable potency, amide non-urea derivatives with oxadiazole ring as a novel secondary pharmacophore against sEH enzyme were developed. Most of the novel compounds with appropriate physical properties, had comparable in vitro sEH inhibitory activity to 12-(3-Adamantan-1-yl-ureido)-dodecanoic acid (AUDA), a potent urea-based sEH inhibitor. The IC50 value of the most potent compound (15c) was 0.43 nM.
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