Substituted pyrazoles as novel sEH antagonist: Investigation of key binding interactions within the catalytic domain
A novel series of pyrazole sEH inhibitors is reported. Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory and microsomal stability profiles.
Lo, Ho Yin,Man, Chuk C.,Fleck, Roman W.,Farrow, Neil A.,Ingraham, Richard H.,Kukulka, Alison,Proudfoot, John R.,Betageri, Raj,Kirrane, Tom,Patel, Usha,Sharma, Rajiv,Hoermann, Mary Ann,Kabcenell, Alisa,Lombaert, Stéphane De
scheme or table
p. 6379 - 6383
(2010/12/19)
SUBSTITUTED PYRAZOLE COMPOUNDS USEFUL AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.
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Page/Page column 122
(2008/06/13)
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