Design, synthesis, and structure–activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF1 receptor antagonists

We designed and synthesized a series of 2-Ar-8-methyl-5-alkylaminolquinolines as potent corticotropin-releasing factor 1 (CRF1) receptor antagonists. The structure–activity relationships of substituents at each position (R3, R5, R5′, and R8) was investigated. By derivatization, three compounds (6, 1...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-09, Vol.22 (17), p.5372-5378
Hauptverfasser:	Takeda, Kunitoshi, Terauchi, Taro, Hashizume, Minako, Shin, Kogyoku, Ino, Mitsuhiro, Shibata, Hisashi, Yonaga, Masahiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals antagonists Biological and medical sciences Corticotropin-releasing factor corticotropin-releasing hormone Depression Depression - drug therapy derivatization Drug Design HEK293 Cells Humans Medical sciences Models, Molecular Pharmacology. Drug treatments Pharmacophore Quinolines - administration & dosage Quinolines - chemical synthesis Quinolines - chemistry Quinolines - pharmacology Rats Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Receptors, Corticotropin-Releasing Hormone - metabolism Stress Structure-Activity Relationship Structure–activity relationships
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Zusammenfassung:	We designed and synthesized a series of 2-Ar-8-methyl-5-alkylaminolquinolines as potent corticotropin-releasing factor 1 (CRF1) receptor antagonists. The structure–activity relationships of substituents at each position (R3, R5, R5′, and R8) was investigated. By derivatization, three compounds (6, 14b, and 14c) were identified as orally active CRF1 receptor antagonists.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.07.047