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

Kunitoshi Takeda; Taro Terauchi; Kogyoku Shin; Mitsuhiro Ino; Hisashi Shibata; Masahiro Yonaga

doi:10.1016/j.bmcl.2012.05.066

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

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4756-61. doi: 10.1016/j.bmcl.2012.05.066. Epub 2012 May 24.

Authors

Kunitoshi Takeda¹, Taro Terauchi, Kogyoku Shin, Mitsuhiro Ino, Hisashi Shibata, Masahiro Yonaga

Affiliation

¹ Medicinal Chemistry, Tsukuba Research Laboratories, Eisai Co., Ltd, 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. k5-takeda@hhc.eisai.co.jp

PMID: 22683343
DOI: 10.1016/j.bmcl.2012.05.066

Abstract

A series of 5-alkylaminolquinolines was designed and synthesized as potential novel CRF(1) receptor antagonists. The structure-activity relationships (SARs) of the substituents on each position (R(2), R(3), R(5) and R(5')) were investigated.

MeSH terms

Alkylation
Amination
Drug Design
HEK293 Cells
Humans
Models, Molecular
Molecular Structure
Quinolines / chemical synthesis*
Quinolines / pharmacology
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Quinolines
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1