Peptidyl-urea based inhibitors of soluble epoxide hydrolases.
Article Details
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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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 4-{[(CYCLOHEXYLAMINO)CARBONYL]AMINO}BUTANOIC ACID Bifunctional epoxide hydrolase 2 IC 50 (nM) 36000 N/A N/A Details 6-{[(CYCLOHEXYLAMINO)CARBONYL]AMINO}HEXANOIC ACID Bifunctional epoxide hydrolase 2 IC 50 (nM) >100000 N/A N/A Details N-[(CYCLOHEXYLAMINO)CARBONYL]GLYCINE Bifunctional epoxide hydrolase 2 IC 50 (nM) >100000 N/A N/A Details