| Title : Symmetric adamantyl-diureas as soluble epoxide hydrolase inhibitors - Burmistrov_2014_Bioorg.Med.Chem.Lett_24_2193 |
| Author(s) : Burmistrov V , Morisseau C , Lee KS , Shihadih DS , Harris TR , Butov GM , Hammock BD |
| Ref : Bioorganic & Medicinal Chemistry Lett , 24 :2193 , 2014 |
|
Abstract :
A series of inhibitors of the soluble epoxide hydrolase (sEH) containing two urea groups has been developed. Inhibition potency of the described compounds ranges from 2.0 muM to 0.4 nM. 1,6-(Hexamethylene)bis[(adamant-1-yl)urea] (3b) was found to be a potent slow tight binding inhibitor (IC50=0.5 nM) with a strong binding to sEH (Ki=3.1 nM) and a moderately long residence time on the enzyme (koff=1.05 x 10(-3) s(-1); t1/2=11 min). |
| PubMedSearch : Burmistrov_2014_Bioorg.Med.Chem.Lett_24_2193 |
| PubMedID: 24685540 |
Burmistrov V, Morisseau C, Lee KS, Shihadih DS, Harris TR, Butov GM, Hammock BD (2014)
Symmetric adamantyl-diureas as soluble epoxide hydrolase inhibitors
Bioorganic & Medicinal Chemistry Lett
24 :2193
Burmistrov V, Morisseau C, Lee KS, Shihadih DS, Harris TR, Butov GM, Hammock BD (2014)
Bioorganic & Medicinal Chemistry Lett
24 :2193