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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 17期

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

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页码：2059 / 2062

页数：4

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