Adamantyl thioureas as soluble epoxide hydrolase inhibitors |
| |
| Authors: | Vladimir Burmistrov Christophe Morisseau Dmitry Pitushkin Dmitry Karlov Robert R Fayzullin Gennady M Butov Bruce D Hammock |
| |
| Institution: | 1. Department of Entomology and Nematology, and Comprehensive Cancer Center, University of California, Davis, CA 95616, USA;2. Department of Chemistry, Technology and Equipment of Chemical Industry, Volzhsky Polytechnic Institute (Branch) Volgograd State Technical University, Volzhsky 404121, Russia;3. Skolkovo Institute of Science and Technology, Skolkovo Innovation Center, Moscow 143026, Russia;4. Department of Chemistry, Lomonosov Moscow State University, Moscow 119991, Russia;5. Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow Region 142432, Russia;6. Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center of Russian Academy of Sciences, Kazan 420088, Russia |
| |
| 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 50?μM to 7.2?nM. 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. |
| |
| Keywords: | Soluble epoxide hydrolase Inhibitor Adamantane Isothiocyanate Thiourea |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
