Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists

A series of 2-heteroaryl-4-arylimidazoles with potent in vitro activity at the NPY5 receptor was developed. Introduction of electron-withdrawing groups on the 4-aryl ring led to a significant improvement of in vitro potency. Several analogues from this series had anorectic activity in rodent feeding...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (20), p.3593-3596
Hauptverfasser:	ELLIOTT, Richard L, OLIVER, Robert M, MACK, Christine M, CASSELLA, James V, LAFLAMME, Janet A, GILLASPY, Melissa L, HAMMOND, Marlys, HANK, Richard F, MAURER, Tristan S, BAKER, Demetria L, DASILVA-JARDINE, Paul A, STEVENSON, Ralph W
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Behavior, Animal - drug effects Biological and medical sciences Feeding Behavior - drug effects Imidazoles - chemistry Imidazoles - pharmacology Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Rats Receptors, Neuropeptide Y - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	A series of 2-heteroaryl-4-arylimidazoles with potent in vitro activity at the NPY5 receptor was developed. Introduction of electron-withdrawing groups on the 4-aryl ring led to a significant improvement of in vitro potency. Several analogues from this series had anorectic activity in rodent feeding models, but were also found to have undesired behavioral effects in spontaneous locomotor activity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00747-9