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.

中文翻译：

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金刚烷硫脲作为可溶性环氧化物水解酶抑制剂

已经开发了一系列含有一个或两个硫脲基团的可溶性环氧化物水解酶（sEH）的抑制剂。所述化合物的抑制能力为50μM至7.2nM。在测试的硫脲中，发现1,7-（七亚甲基）双[（金刚烷基-1-基）硫脲]（6f）是最有效的sEH抑制剂。硫脲对人sEH的抑制作用更接近于对大鼠sEH的抑制作用，而不是对鼠sEH的抑制作用。尽管硫脲的活性较低，但其溶解度却比尿素高7倍，这使其具有更高的生物利用度，因此有望用作sEH抑制剂。