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 models, but were also found to have undesired behavioral effects in spontaneous locomotor activity.
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D005247:Feeding Behavior / Q000187:drug effects; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D007093:Imidazoles; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor