Discovery and SAR of novel [1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK)

被引：46
|
作者：
Cywin, CL
Zhao, BP
McNeil, DW
Hrapchak, M
Prokopowicz, AS
Goldberg, DR
Morwick, TM
Gao, A
Jakes, S
Kashem, M
Magolda, RL
Soll, RM
Player, MR
Bobko, MA
Rinker, J
DesJarlais, RL
Winters, MP
机构：
[1] Boehringer Ingelheim Pharmaceut Inc, Ridgefield, CT 06801 USA
[2] 3 Dimens Pharmaceut Inc, Exton, PA 19341 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 08期
关键词：
D O I：
10.1016/S0960-894X(03)00163-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity for a 7-aryl group with preference towards para substitution and that this in combination with 5-aminoalkylamino substituents further improved the potency of the compounds. The initial SAR as well as a survey of the other positions is discussed in detail. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1415 / 1418
页数：4
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