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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (20), p.3593-3596
Main Authors: 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: Article
Language:English
Subjects:
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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Summary: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