Title of article
Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase
Author/Authors
Paul D. Jones، نويسنده , , Hsing-Ju Tsai، نويسنده , , Zung N. Do، نويسنده , , Christophe Morisseau، نويسنده , , Bruce D. Hammock، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5212
To page
5216
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.
Keywords
Soluble epoxide hydrolase , enzyme inhibition , Structure–activity relationships
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797359
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