| Title : Adamantyl thioureas as soluble epoxide hydrolase inhibitors - Burmistrov_2018_Bioorg.Med.Chem.Lett_28_2302 |
| Author(s) : Burmistrov V , Morisseau C , Pitushkin D , Karlov D , Fayzullin RR , Butov GM , Hammock BD |
| Ref : Bioorganic & Medicinal Chemistry Lett , 28 :2302 , 2018 |
|
Abstract :
A series of inhibitors of the soluble epoxide hydrolase (sEH) containing one or two thiourea groups has been developed. Inhibition potency of the described compounds ranges from 50muM to 7.2nM. 1,7-(Heptamethylene)bis[(adamant-1-yl)thiourea] (6f) was found to be the most potent sEH inhibitor, among the thioureas tested. The inhibitory activity of the thioureas against the human sEH is closer to the value of activity against rat sEH rather than murine sEH. While being less active, thioureas are up to 7-fold more soluble than ureas, which makes them more bioavailable and thus promising as sEH inhibitors. |
| PubMedSearch : Burmistrov_2018_Bioorg.Med.Chem.Lett_28_2302 |
| PubMedID: 29803731 |
Burmistrov V, Morisseau C, Pitushkin D, Karlov D, Fayzullin RR, Butov GM, Hammock BD (2018)
Adamantyl thioureas as soluble epoxide hydrolase inhibitors
Bioorganic & Medicinal Chemistry Lett
28 :2302
Burmistrov V, Morisseau C, Pitushkin D, Karlov D, Fayzullin RR, Butov GM, Hammock BD (2018)
Bioorganic & Medicinal Chemistry Lett
28 :2302