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Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase |
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| 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 |
| Institution: | 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 |
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