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Title: Fluoroaromatic fragments on 1,3-disubstituted ureas enhance soluble epoxide hydrolase inhibition.

Authors: Burmistrov, Vladimir; Morisseau, Christophe; D'yachenko, Vladimir; Rybakov, Victor B; Butov, Gennady M; Hammock, Bruce D

Published In J Fluor Chem, (2019 Apr)

Abstract: A series of soluble epoxide hydrolase (sEH) inhibitors containing 2-fluorophenyl fragment was developed. Inhibition potency of the described compounds ranges from 0.7 to 630.9 nM. 1-(Adamantan-1-ylmethyl)-3-(2-fluorophenyl) urea (3b, IC50 = 0.7 nM) and 1-(adamantan-2-yl)-3-(2-fluorophenyl) urea (3i, IC50 =1.0 nM) were found to be the most potent sEH inhibitors within the described series. Crystal results suggest that potency is probably enhanced by extra hydrogen bond between the fluorine atom and catalytic tyrosine residues.

PubMed ID: 32132741 Exiting the NIEHS site

MeSH Terms: No MeSH terms associated with this publication

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