Design and synthesis of new prostaglandin D2 receptor antagonists

被引：3

作者：

Iwahashi, Maki ^{[1
]}

Takahashi, Eiji ^{[2
]}

Tanaka, Motoyuki ^{[1
]}

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, Qual Assurance Headquarters, Tsukuba, Ibaraki 3004247, Japan

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 18期

关键词：

Prostaglandin; DP receptor; Antagonist; Phenylacetic acid; AMIDE STRUCTURE; HUMAN-SKIN; DISCOVERY; PHARMACOLOGY; SUBTYPES; POTENT; RAT;

D O I：

10.1016/j.bmc.2011.08.007

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 cost-effective prostaglandin D-2 (DP) receptor antagonists, a series of novel 3-benzoylaminophenylacetic acids were synthesized and biologically evaluated. Among those tested, some representative compounds were found to be orally available. Receptor selectivity and rat PK profiles were also evaluated. The structure-activity relationship (SAR) study is presented. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5361 / 5371

页数：11

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