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Bioorg Med Chem Lett. 2003 Oct 20;13(20):3593-6.

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

Author information

1
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.

PMID:
14505677
DOI:
10.1016/s0960-894x(03)00747-9
[Indexed for MEDLINE]

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