Design, synthesis and structure-activity relationships of 5-alkylaminolquinolines as a novel series of CRF1 receptor antagonists.
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.
Medicinal Chemistry, Tsukuba Research Laboratories, Eisai Co., Ltd, 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. k5-takeda@hhc.eisai.co.jp
Kunitoshi
K
Takeda
Taro
T
Terauchi
Kogyoku
K
Shin
Mitsuhiro
M
Ino
Hisashi
H
Shibata
Masahiro
M
Yonaga
D000478:Alkylation; D000586:Amination; D015195:Drug Design; D057809:HEK293 Cells; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000099052:CRF Receptor, Type 1
D011804:Quinolines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1