Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists

被引：15

作者：

Saito, Tetsuji ^{[1
]}

Obitsu, Tetsuo ^{[1
]}

Kohno, Hiroshi ^{[1
]}

Sugimoto, Isamu ^{[1
]}

Matsushita, Takeshi ^{[1
]}

Nishiyama, Taihei ^{[1
]}

Hirota, Tomoko ^{[1
]}

Takeda, Hiroyuki ^{[1
]}

Matsumura, Naoya ^{[1
]}

Ueno, Sonoko ^{[1
]}

Kishi, Akihiro ^{[1
]}

Kagamiishi, Yoshifumi ^{[1
]}

Nakai, Hisao ^{[1
]}

Takaoka, Yoshikazu ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 02期

关键词：

Corticotropin-releasing factor 1 receptor; Antagonist; MAJOR DEPRESSION; HORMONE; ANXIETY; DMP696; DERIVATIVES; R121919; SYSTEM;

D O I：

10.1016/j.bmc.2011.11.015

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 structurally novel corticotropin-releasing factor 1 (CRF1) receptor antagonists, a series of bicyclic core analogs pyrrolo[1,2-b]pyridazines and pyrrolo[2,1-f]triazin-4(3H)-ones, which were designed based on a monocyclic core antagonist, was synthesized and evaluated. Among the compounds tested, 2-difluoromethoxy-4-methylpyridin-5-yl analog 27 was found to show efficacy in a dose-dependent manner in an elevated plus maze test in rats. The discovery process and structure-activity relationship is presented. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1122 / 1138

页数：17

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