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ID: ALA1154229

Journal: Bioorg Med Chem Lett

Title: Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.

Authors: Shen HC, Ding FX, Deng Q, Xu S, Chen HS, Tong X, Tong V, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Zhang B, Roy S, Tata JR, Berger JP, Colletti SL.

Abstract: 3,3-Disubstituted piperidine-derived trisubstituted urea entA-2b was discovered as a highly potent and selective soluble epoxide hydrolase (sEH) inhibitor. Despite the good compound oral exposure, excellent sEH inhibition in whole blood, and remarkable selectivity, compound entA-2b failed to lower blood pressure acutely in spontaneously hypertensive rats (SHRs). This observation further challenges the premise that sEH inhibition can provide a viable approach to the treatment of hypertensive patients.

CiteXplore: 19682899

DOI: 10.1016/j.bmcl.2009.07.138