Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists

被引:15
|
作者
Wilcoxen, K
Huang, CQ
McCarthy, JR
Grigoriadis, DE
Chen, C
机构
[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92121 USA
[2] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92121 USA
关键词
D O I
10.1016/S0960-894X(03)00621-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
3-Phenylpyrazolo[4,3-b]pyridines were synthesized via a cyclization of 4-amino-3-phenylpyrazoles 11-13 with ethyl acetoacetate. These compounds were found to be potent CRF1 antagonists. The 2-alkylpyrazolo[4,3-b]pyridines were more polar but less active than the corresponding 1-alkyl-isomers. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3367 / 3370
页数:4
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