Discovery of selective indole-based prostaglandin D2 receptor antagonist

被引：10

作者：

Iwahashi, Maki ^{[1
]}

Shimabukuro, Atsushi ^{[1
]}

Onoda, Takahiro ^{[2
]}

Matsunaga, Yoko ^{[1
]}

Okada, Yutaka ^{[1
]}

Matsumoto, Ryoji ^{[3
]}

Nambu, Fumio ^{[1
]}

Nakai, Hisao ^{[1
]}

Toda, Masaaki ^{[1
]}

机构：

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

[2] Ono Pharmaceut Co Ltd, Fukui Res Inst, Fukui 9138538, Japan

[3] Ono Pharmaceut Co Ltd, Osaka 5418526, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 15期

关键词：

Prostaglandin; DP receptor; Antagonist; Indole; BIOLOGICAL-ACTIVITY; BASAL FOREBRAIN; HUMAN-SKIN; POTENT; DERIVATIVES; SERIES; ROLES; SLEEP; CELLS; CRTH2;

D O I：

10.1016/j.bmc.2011.06.014

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 N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D-2 receptor antagonists. Some of the selected compounds significantly inhibited OVA-induced vascular permeability in guinea pig conjunctiva after oral dosing. Structure-activity relationship study is presented. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：4574 / 4588

页数：15

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