Design, synthesis and structure-activity relationships of 5-alkylaminolquinolines as a novel series of CRF1 receptor antagonists

被引：7

作者：

Takeda, Kunitoshi ^{[1
]}

Terauchi, Taro ^{[1
]}

Shin, Kogyoku ^{[1
]}

Ino, Mitsuhiro ^{[2
]}

Shibata, Hisashi ^{[2
]}

Yonaga, Masahiro ^{[1
]}

机构：

[1] Eisai & Co Ltd, Tsukuba Res Labs, Med Chem, Tsukuba, Ibaraki 3002635, Japan

[2] Eisai & Co Ltd, Tsukuba Res Labs, Biopharmacol, Tsukuba, Ibaraki 3002635, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 14期

关键词：

CRF; SAR; Pharmacophore; Stress; Depression; CORTICOTROPIN-RELEASING-FACTOR; TYPE-1; RECEPTOR; EXPRESSION; CLONING; POTENT; CP-154,526; BINDING; STRESS; BRAIN;

D O I：

10.1016/j.bmcl.2012.05.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5-alkylaminolquinolines was designed and synthesized as potential novel CRF1 receptor antagonists. The structure-activity relationships (SARs) of the substituents on each position (R-2, R-3, R-5 and R-5') were investigated. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：4756 / 4761

页数：6

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