A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors |
| |
| Authors: | Schlapbach Achim Heng Richard Di Padova Franco |
| |
| Institution: | Novartis Institute for Biomedical Research, Arthritis and Bone Metabolism, Lichtstrasse, CH-4002, Basel, Switzerland. achim.schlapbach@pharma.novartis.com |
| |
| Abstract: | A series of potent p38 inhibitors based on the dihydroquinazoline scaffold was synthesized using a novel Pd-catalyzed cyclization reaction of aryl-benzyl ureas. Optimization of this compound class led to compound 20, which inhibits p38alpha in vitro with IC(50)=14 nM and is active in the mouse TNFalpha-release model. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
