期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 4, 页码 1066-1070出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.013
关键词
sEH inhibitors; Non-urea; Primary pharmacophore
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. (C) 2009 Elsevier Ltd. All rights reserved.
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