Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 19, Pages 5212-5216Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.07.009
Keywords
soluble epoxide hydrolase; enzyme inhibition; structure-activity relationships
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Funding
- NHLBI NIH HHS [R01 HL059699, F32 HL078096, R01 HL59699-06A1] Funding Source: Medline
- NIEHS NIH HHS [R01 ES002710, P42 ES04699, ES02710, P42 ES004699, R37 ES002710] Funding Source: Medline
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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 mu M to 1.1 nM against recombinant sEH. N-(1 -Acetylpiperidin-4-yi)N'-(adamant-1-yl) urea (5a) was found to be a potent inhibitor (IC50 = 7.0 nM) that was also orally bioavailable in canines. (c) 2006 Elsevier Ltd. All rights reserved.
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