Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists

The synthesis and biological optimization for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-04, Vol.17 (7), p.2031-2035
Hauptverfasser:	Madsen-Duggan, Christina B., Debenham, John S., Walsh, Thomas F., Toupence, Richard B., Huang, Song X., Wang, Junying, Tong, Xinchun, Lao, Julie, Fong, Tung M., Schaeffer, Marie-Therese, Xiao, Jing Chen, Huang, Cathy R.-R.C., Shen, Chun-Pyn, Stribling, D. Sloan, Shearman, Lauren P., Strack, Alison M., MacIntyre, D. Euan, Van der Ploeg, Lex H.T., Goulet, Mark T.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Behavior, Animal - drug effects Biological and medical sciences Cannabinoid CB1 Chemistry, Pharmaceutical - methods Drug Design Feeding Behavior - drug effects General and cellular metabolism. Vitamins Inhibitory Concentration 50 Inverse agonist Medical sciences Miscellaneous Models, Chemical Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Obesity Pharmacology. Drug treatments Pyridine Pyridines - chemical synthesis Pyridines - chemistry Rats Rats, Sprague-Dawley Receptor, Cannabinoid, CB1 - agonists Structure-Activity Relationship Temperature Toluene - chemistry
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The synthesis and biological optimization for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.01.005