|
|||||
|
|
Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists |
|
| Authors: | Elliott Richard L Oliver Robert M LaFlamme Janet A Gillaspy Melissa L Hammond Marlys Hank Richard F Maurer Tristan S Baker Demetria L DaSilva-Jardine Paul A Stevenson Ralph W Mack Christine M Cassella James V |
| Affiliation: | Department of Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. richard_l_elliott@groton.pfizer.com |
| Abstract: | 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. |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |