|
|||||
|
|
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase |
|
| Authors: | Hammach Abdelhakim Barbosa Antonio Gaenzler Faith Corbo Fadra Tazmeen Goldberg Daniel Hao Ming-Hong Kroe Rachel R Liu Pingrong Qian Kevin C Ralph Mark Sarko Christopher Soleymanzadeh Fariba Moss Neil |
| Affiliation: | aDepartments of Medicinal Chemistry and Biologics and Biomolecular Sciences, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA |
| Abstract: | A new class of benzimidazolone p38 MAP kinase inhibitors was discovered through high-throughput screening. X-ray crystallographic data of the lead molecule with p38 were used to design analogues with improved binding affinity and potency in a cell assay of LPS-induced TNF production. Herein, we report the SAR of this new class of p38 inhibitors. |
| Keywords: | p38 MAP kinase Inhibitor Benzimidazolone |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |