Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists

被引：23

作者：

Asada, Masaki ^{[1
]}

Obitsu, Tetsuo ^{[1
]}

Kinoshita, Atsushi ^{[1
]}

Nakai, Yoshihiko ^{[1
]}

Nagase, Toshihiko ^{[1
]}

Sugimoto, Isamu ^{[1
]}

Tanaka, Motoyuki ^{[1
]}

Takizawa, Hiroya ^{[1
]}

Yoshikawa, Ken ^{[1
]}

Sato, Kazutoyo ^{[1
]}

Narita, Masami ^{[1
]}

Ohuchida, Shuichi ^{[1
]}

Nakai, Hisao ^{[1
]}

Toda, Masaaki ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 08期

关键词：

Prostaglandin; EP3; receptor; Antagonist; N-Acylsulfonamide; N-Acyl (3,4-difluorobenzene)sulfonamide; PROSTANOID RECEPTOR; MICE LACKING; SUBTYPE; MYOMETRIUM;

D O I：

10.1016/j.bmcl.2010.02.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE(2)-induced uterine contraction in pregnant rats. Among those tested, a series of N-acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed. (C) 2010 Published by Elsevier Ltd.

引用

页码：2639 / 2643

页数：5

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