CONFORMATIONALLY RESTRICTED UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE
Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
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Page/Page column 23
(2008/06/13)
Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase
A series of conformationally restricted inhibitors of human soluble epoxide hydrolase (sEH) has been developed. Inhibition potency of the described compounds ranges from 4.2 μM to 1.1 nM against recombinant sEH. N-(1-Acetylpiperidin-4-yl)-N′-(adamant-1-yl) urea (5a) was found to be a potent inhibitor (IC50 = 7.0 nM) that was also orally bioavailable in canines.
Jones, Paul D.,Tsai, Hsing-Ju,Do, Zung N.,Morisseau, Christophe,Hammock, Bruce D.
p. 5212 - 5216
(2008/02/03)
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