Pyridazine based inhibitors of p38 MAPK |
| |
| Authors: | McIntyre Charles J Ponticello Gerald S Liverton Nigel J O'Keefe Stephen J O'Neill Edward A Pang Margaret Schwartz Cheryl D Claremon David A |
| |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. mcintyre@merck.com |
| |
| Abstract: | Trisubstituted pyridazines were synthesized and evaluated as in vitro inhibitors of p38MAPK. The most active isomers were those possessing an aryl group alpha and a heteroaryl group beta relative to the nitrogen atom in the 2-position of the central pyridazine. Additionally, substitution in the 6-position of the central pyridazine with a variety of dialkylamino substituents afforded a set of inhibitors having good (p38 IC50 1-20 nM) in vitro activity. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
