Article,

Synthesis and \SAR\ of conformationally restricted inhibitors of soluble epoxide hydrolase

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Bioorganic & Medicinal Chemistry Letters, 16 (19): 5212 - 5216 (2006)
DOI: https://doi.org/10.1016/j.bmcl.2006.07.009

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 μM 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 (IC50 = 7.0 nM) that was also orally bioavailable in canines.

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