Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists

A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF1R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein. A novel series of [6-chloro-2-trifluoromethyl...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-06, Vol.20 (12), p.3669-3674
Hauptverfasser:	Zuev, Dmitry, Vrudhula, Vivekananda M., Michne, Jodi A., Dasgupta, Bireshwar, Pin, Sokhom S., Huang, Xiaohua Stella, Wu, Dedong, Gao, Qi, Zhang, Jie, Taber, Matthew T., Macor, John E., Dubowchik, Gene M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anxiety Biological and medical sciences Corticotropin-releasing factor Depression Hormones. Endocrine system Humans Imidazoles - chemistry Imidazoles - pharmacology Medical sciences Methylamines - chemistry Methylamines - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Parallel synthesis Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Protein Binding Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF1R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein. A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF1R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.04.094