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ID: ALA1146911

Journal: Bioorg Med Chem Lett

Title: Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase.

Authors: Jones PD, Tsai HJ, Do ZN, Morisseau C, Hammock BD.

Abstract: A series of conformationally restricted inhibitors of human soluble epoxide hydrolase (sEH) has been developed. Inhibition potency of the described compounds ranges from 4.2 microM to 1.1 nM against recombinant sEH. N-(1-Acetylpiperidin-4-yl)-N'-(adamant-1-yl) urea (5a) was found to be a potent inhibitor (IC(50) = 7.0 nM) that was also orally bioavailable in canines.

CiteXplore: 16870439

DOI: 10.1016/j.bmcl.2006.07.009