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Bioorg Med Chem Lett. 2007 Sep 15;17(18):5245-50. Epub 2007 Jun 30.

Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

Author information

1
Department of Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. jennifer.lafontaine@pfizer.com

Abstract

A novel series of heterocycle-based analogs were prepared and evaluated for their in vitro and in vivo biological activity as human beta(3)-adrenergic receptor (AR) agonists. Several analogs demonstrated potent agonist activity at the beta(3)-AR, functional selectivity against beta(1)- and beta(2)-ARs, and favorable pharmacokinetic profiles in vivo. Compound 17 increased oxygen consumption in rats, a measure of energy expenditure, with an ED(20%) of 2mg/kg.

PMID:
17632003
DOI:
10.1016/j.bmcl.2007.06.072
[Indexed for MEDLINE]

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