Ontology highlight
ABSTRACT:
SUBMITTER: Burmistrov V
PROVIDER: S-EPMC4019751 | biostudies-literature | 2014 May
REPOSITORIES: biostudies-literature
Burmistrov Vladimir V Morisseau Christophe C Lee Kin Sing Stephen KS Shihadih Diyala S DS Harris Todd R TR Butov Gennady M GM Hammock Bruce D BD
Bioorganic & medicinal chemistry letters 20140320 9
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). ...[more]