SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors

被引:121
作者
Liu, LP
Stelmach, JE
Natarajan, SR
Chen, MH
Singh, SB
Schwartz, CD
Fitzgerald, CE
O'Keefe, SJ
Zaller, DM
Schmatz, DM
Doherty, JB
机构
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Inflamat Res, Rahway, NJ 07065 USA
关键词
D O I
10.1016/j.bmcl.2003.08.059
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Development for a class of potent 3,4-dihydropyrido(3,2-d)pyrimidone inhibitors of p38a MAP kinase is described. Modification of N-1 aryl and C-6 arylsulfide in 3,4-dihydropyrido (3,2-d)pyrimidone analogues for the interaction with the hydrophobic pockets in p38 active site is also discussed. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3979 / 3982
页数:4
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