Discovery of FK453, a novel non-xanthine adenosine A(1) receptor antagonist

被引:27
作者
Akahane, A
Katayama, H
Mitsunaga, T
Kita, Y
Kusunoki, T
Terai, T
Yoshida, K
Shiokawa, Y
机构
[1] New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Kashima, Yodogawa-ku, Osaka 532, 1-6
关键词
D O I
10.1016/0960-894X(96)00368-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel 2-phenylpyrazolo[1,5-a]pyridine-3-acryloylamides were synthesized and evaluated for diuretic activities. FK453 (1d), the most potent compound in this series, was found to be a potent and selective adenosine A(1) receptor antagonist, whereas 1e, the (S)-enantiomer of FK453, was a weak and non-selective adenosine antagonist. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:2059 / 2062
页数:4
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