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

✍ Scribed by Richard L. Elliott; Robert M. Oliver; Janet A. LaFlamme; Melissa L. Gillaspy; Marlys Hammond; Richard F. Hank; Tristan S. Maurer; Demetria L. Baker; Paul A. DaSilva-Jardine; Ralph W. Stevenson; Christine M. Mack; James V. Cassella

Publisher
Elsevier Science
Year
2003
Tongue
English
Weight
142 KB
Volume
13
Category
Article
ISSN
0960-894X

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✦ Synopsis

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.

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