Substituted pyrazoles as novel sEH antagonist: Investigation of key binding interactions within the catalytic domain

Ho Yin Lo,Chuk C. Man,Roman W. Fleck,Neil A. Farrow,Richard H. Ingraham,Alison Kukulka,John R. Proudfoot,Raj Betageri,Tom Kirrane,Usha Patel,Rajiv Sharma,Mary Ann Hoermann,Alisa Kabcenell,Stéphane De Lombaert

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

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.

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关键词

sEH,Pyrazoles,Aniline,EETs,Anti-hypertension

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