Salicylate-urea-based soluble epoxide hydrolase inhibitors with high metabolic and chemical stabilities

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:19

Article

Morisseau, Christophe¹ 

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

关键词: Soluble epoxide hydrolase;    Urea;    Salicylate;    Intramolecular hydrogen bond;    Metabolic and chemical stability;    Hypertension;    Anti-inflammation;   

DOI  :  10.1016/j.bmcl.2009.01.069

来源: Elsevier

【 摘 要 】

We investigated N-adamantyl-N'-phenyl urea derivatives as simple sEH inhibitors. Salicylate ester derivatives have high inhibitory activities against human sEH, while the free benzoic acids are less active. The methyl salicylate derivative is a potent sEH inhibitor, which also has high metabolic and chemical stabilities; suggesting that such inhibitors are potential lead molecule for bioactive compounds acting in vivo. (C) 2009 Elsevier Ltd. All rights reserved.

【 授权许可】

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