Non-urea functionality as the primary pharmacophore in soluble epoxide hydrolase inhibitors |
| |
Authors: | Sampath-Kumar Anandan Zung N. Do Heather K. Webb Dinesh V. Patel Richard D. Gless |
| |
Affiliation: | Arête Therapeutics, Inc., 3912 Trust Way, Hayward, CA 94545, USA |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|