Design and synthesis of a selective EP4-receptor agonist.: Part 2:: 3,7-dithiaPGE1 derivatives with high selectivity

被引：11

作者：

Maruyama, T ^{[1
]}

Asada, M ^{[1
]}

Shiraishi, T ^{[1
]}

Ishida, A ^{[1
]}

Yoshida, H ^{[1
]}

Maruyama, T ^{[1
]}

Ohuchida, S ^{[1
]}

Nakai, H ^{[1
]}

Kondo, K ^{[1
]}

Toda, M ^{[1
]}

机构：

[1] Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 04期

关键词：

D O I：

10.1016/S0968-0896(01)00352-2

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：

To identify new highly selective EP4-agonists, further modification of the 16-phenyl moiety of 1 was continued. 16-(3-Methoxymethyl)phenyl derivatives 13-(6q) and 16-(3-ethoxymethyl)phenyl derivatives 13-(7c), showed more selectivity and potent agonist activity than 1. 16-(3-Methyl-4-hydroxy)phenyl derivative 18-(14e) demonstrated excellent subtype selectivity, while both its receptor affinity and agonist activity were less potent than those of 13-(6q), Structure-activity relationships (SARs) are also discussed. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：989 / 1008

页数：20

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