Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 28, Issue 13, Pages 2302-2313Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.05.024
Keywords
Soluble epoxide hydrolase; Inhibitor; Adamantane; Isothiocyanate; Thiourea
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Funding
- Russian Fund for Basic Research [16-33-00172]
- Ministry of Education and Science of the Russian Federation [4.7491.2017/BCh]
- National Institute of Environmental Health Sciences (NIEHS) [R01 ES002710]
- NIEHS Superfund Research Program [P42 ES004699]
- NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES [P42ES004699, R01ES002710] Funding Source: NIH RePORTER
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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 mu M to 7.2 nM. 1,7-(Heptamethylene) bisRadamant-1-yl)thioureal (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.
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