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Updated: Jun 26, 2026

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase
Published on: November 23, 2016
Non-urea functionality as the primary pharmacophore in soluble epoxide hydrolase inhibitors
Sampath-Kumar Anandan1, Zung N Do, Heather K Webb
1Arête Therapeutics, Inc., 3912 Trust Way, Hayward, CA 94545, USA. skumar@aretetherapeutics.com
Abstract:
Inhibition of soluble epoxide hydrolase has been proposed as a promising new pharmaceutical target for diseases involving hypertension and vascular inflammation. The most potent sEH inhibitors reported to date contain a urea or amide moiety as the central or 'primary' pharmacophore. We evaluated replacing the urea pharmacophore with other functional groups such as thiourea, sulfonamide, sulfonylurea, aminomethylene amide, hydroxyamide, and ketoamide to identify novel and potent inhibitors. The hydroxyamide moiety was identified as a novel pharmacophore affording potency comparable to urea.
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