Design, synthesis and evaluation of non-urea inhibitors of soluble epoxide hydrolase

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Pecic, Stevan¹  Deng, Shi-Xian¹  Morisseau, Christophe^2,3  Hammock, Bruce D.^2,3  Landry, Donald W.¹ 

[1] Columbia Univ, Dept Med, New York, NY 10032 USA

[2] Univ Calif Davis, Dept Entomol, Davis, CA 95616 USA

[3] Univ Calif Davis, UCD Canc Ctr, Davis, CA 95616 USA

关键词: Soluble epoxide hydrolase;    sEH;    Non-urea inhibitors;    Hypertension;    Anti-inflamatory;   

DOI  :  10.1016/j.bmcl.2011.10.074

来源: Elsevier

【 摘 要 】

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. Published by Elsevier Ltd.

【 授权许可】

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