|
|||||
|
|
Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain |
|
| Authors: | 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 |
| Affiliation: | 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. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |