Synthesis and structure-activity relationships of a new class of selective EP3 receptor agonist, 13,14-didehydro-16-phenoxy analogues of prostaglandin E1

被引:12
作者
Shimazaki, Y
Kameo, K
Tanami, T
Tanaka, H
Ono, N
Kiuchi, Y
Okamoto, S
Sato, F
Ichikawa, A
机构
[1] Taisho Pharmaceut Co Ltd, Med Res Ctr, Ohmiya, Saitama 3308530, Japan
[2] Tokyo Inst Technol, Dept Biomol Engn, Midori Ku, Kanagawa 2268501, Japan
[3] Kyoto Univ, Fac Pharmaceut Sci, Dept Physiol Chem, Sakyo Ku, Kyoto 6068501, Japan
关键词
prostaglandins; agonists; receptors; substituent effects;
D O I
10.1016/S0968-0896(99)00288-6
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of 13,14-didehydro-16-phenoxy analogues of prostaglandin E-1 was synthesized and their agonistic activity on EP receptor subtypes was evaluated. 13,14-Didehydro-16-phenoxy-1-decarboxy analogues, 7e and 7f, display highly selective activity on the EP3 receptor subtype, thus, their utility as a selective anti-ulcer agent can be expected. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:353 / 362
页数:10
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