Peptidyl-urea based inhibitors of soluble epoxide hydrolases |
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Authors: | Morisseau Christophe Newman John W Tsai Hsing-Ju Baecker Preston A Hammock Bruce D |
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Institution: | Department of Entomology and UCD Cancer Center, University of California, Davis, CA 95616, USA. |
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Abstract: | We prepared a series of amino acid derived cyclohexyl and adamantyl ureas and tested them as inhibitors of the human soluble epoxide hydrolase, and obtained very potent compounds (K(I)=15nM) that are >10-fold more soluble than previously described sEH inhibitors. While our lead compound 2 showed low apparent bioavailability in dogs and rats, this series of compounds revealed that sEH inhibitor structures could accept large groups that could lead to better orally available drugs. |
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