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- Title
Design, Synthesis and Biological Activity of 4,6-disubstituted Pyridin- 2(1H)-ones as Novel Inhibitors of Soluble Epoxide Hydrolase.
- Authors
Hejazi, Leila; Rezaee, Elham; Tabatabai, Sayyed Abbas
- Abstract
Soluble epoxide hydrolase enzyme is a promising therapeutic target for hypertension, vascular inflammation, pain and some other risk factors of cardiovascular diseases. The most potent sEH inhibitors reported in the literature are urea-based ones which often have poor bioavailability. In this study, in a quest for finding potent inhibitors of soluble epoxide hydrolase, some 4,6-disubstituted pyridin-2(1H)-one derivatives were designed and synthesized. The designed compounds fit properly in the active site pocket of this enzyme in docking studies and have appropriate distances for effective hydrogen binding to important amino acids Tyr383, Tyr466, and Asp335. The results of biological evaluation of these compounds against soluble epoxide hydrolase enzyme indicate most compounds have acceptable inhibitory activity and compound 9c is the most potent inhibitor with inhibitory activity of 86%.
- Subjects
EPOXIDE hydrolase; BIOSYNTHESIS; BINDING sites; DISEASE risk factors; ANGIOTENSIN I
- Publication
Iranian Journal of Pharmaceutical Research, 2019, Vol 18, Issue 4, p1759
- ISSN
1735-0328
- Publication type
Article
- DOI
10.22037/ijpr.2019.112047.13500