Discovery of 6-Oxo-3-(2-phenylpyrazolo [1, 5-a] pyridin-3-yl)-1 (6 H)-pyridazinebutanoic Acid (FK 838): A Novel Non-Xanthine Adenosine A1 Receptor Antagonist with …

A Akahane, H Katayama, T Mitsunaga…

Index: Akahane, Atsushi; Katayama, Hirohito; Mitsunaga, Takafumi; Kato, Takeshi; Kinoshita, Takayoshi; Kita, Yasuhiro; Kusunoki, Takahiro; Terai, Takao; Yoshida, Keizo; Shiokawa, Youichi Journal of Medicinal Chemistry, 1999 , vol. 42, # 5 p. 779 - 783

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Citation Number: 105

Abstract

Design. In structure− activity relationship (SAR) studies of 2, the (E)-acryloyl moiety was found to be indispensable for potent diuretic activity (unpublished results). Compounds in which the (E)-acryloyl moiety was replaced by (Z)-acryloyl, propionyl, or propioloyl were essentially inactive. Therefore, it was quite clear that the conformation of the acryloyl part of 2 was very important. The X-ray crystal structure of 2 (Figure 2) clearly indicated that the (E ...