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Title: Symmetric adamantyl-diureas as soluble epoxide hydrolase inhibitors.

Authors: Burmistrov, Vladimir; Morisseau, Christophe; Lee, Kin Sing Stephen; Shihadih, Diyala S; Harris, Todd R; Butov, Gennady M; Hammock, Bruce D

Published In Bioorg Med Chem Lett, (2014 May 1)

Abstract: A series of inhibitors of the soluble epoxide hydrolase (sEH) containing two urea groups has been developed. Inhibition potency of the described compounds ranges from 2.0 μM to 0.4 nM. 1,6-(Hexamethylene)bis[(adamant-1-yl)urea] (3b) was found to be a potent slow tight binding inhibitor (IC50=0.5 nM) with a strong binding to sEH (Ki=3.1 nM) and a moderately long residence time on the enzyme (koff=1.05 × 10(-3) s(-1); t1/2=11 min).

PubMed ID: 24685540 Exiting the NIEHS site

MeSH Terms: Adamantane/analogs & derivatives*; Adamantane/pharmacology*; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Epoxide Hydrolases/antagonists & inhibitors*; Epoxide Hydrolases/metabolism; Humans; Molecular Docking Simulation; Urea/analogs & derivatives*; Urea/pharmacology*

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