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 CRF1 receptor antagonists. The structure–activity relationships (SARs) of the substituents on each position (R2, R3, R5 and R5′) were investigated.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-07, Vol.22 (14), p.4756-4761
Hauptverfasser:	Takeda, Kunitoshi, Terauchi, Taro, Shin, Kogyoku, Ino, Mitsuhiro, Shibata, Hisashi, Yonaga, Masahiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Amination antagonists Biological and medical sciences CRF Depression Drug Design HEK293 Cells Humans Medical sciences Models, Molecular Molecular Structure Neuropharmacology Pharmacology. Drug treatments Pharmacophore Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology quinolines Quinolines - chemical synthesis Quinolines - pharmacology receptors Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors SAR Stress Structure-Activity Relationship structure-activity relationships
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Beschreibung
Zusammenfassung:	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 (R2, R3, R5 and R5′) were investigated.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.05.066