Peptidyl-urea based inhibitors of soluble epoxide hydrolases.
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Morisseau C, Newman JW, Tsai HJ, Baecker PA, Hammock BD
Peptidyl-urea based inhibitors of soluble epoxide hydrolases.
Bioorg Med Chem Lett. 2006 Oct 15;16(20):5439-44.
- PubMed ID
- 16908134 [ View in PubMed]
- 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.