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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6379-83. doi: 10.1016/j.bmcl.2010.09.095. Epub 2010 Sep 19.

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

Author information

1
Boehringer Ingelheim Pharmaceuticals Inc., Biomolecular Screening, 900 Ridgebury Rd., PO Box 368, Ridgefield, CT 06877, USA. ho-yin.lo@boehringer-ingelheim.com

Abstract

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.

PMID:
20934334
DOI:
10.1016/j.bmcl.2010.09.095
[Indexed for MEDLINE]

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