title: Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase.
abstract: Inhibition of soluble epoxide hydrolase (sEH) has been proposed as a new pharmaceutical approach for treating hypertension and vascular inflammation. The most potent sEH inhibitors reported in literature to date are urea derivatives. However, these compounds have limited pharmacokinetic profiles. We investigated non-urea amide derivatives as sEH inhibitors and identified a potent human sEH inhibitor 14-34 having potency comparable to urea-based inhibitors.
authors.affiliation: Department of Medicine, Columbia University, 650 W 168th Street, BB 1029, New York, NY 10032, USA. ar2230@columbia.edu
authors.forename: Stevan
authors.initials: S
authors.lastname: Pecic
authors.forename: Shi-Xian
authors.initials: SX
authors.lastname: Deng
authors.forename: Christophe
authors.initials: C
authors.lastname: Morisseau
authors.forename: Bruce D
authors.initials: BD
authors.lastname: Hammock
authors.forename: Donald W
authors.initials: DW
authors.lastname: Landry
mesh_terms: D000577:Amides / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors*; D005456:Fluorescent Dyes / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D006973:Hypertension / Q000188:drug therapy; D007249:Inflammation / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D008856:Microscopy, Fluorescence / Q000379:methods; D008956:Models, Chemical; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D004851:Epoxide Hydrolases
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