4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 22, Pages 6379-6383

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.095

Keywords

sEH; Pyrazoles; Aniline; EETs; Anti-hypertension

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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. (C) 2010 Elsevier Ltd. All rights reserved.

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