Biarylaniline phenethanolamines as potent and selective β3 adrenergic receptor agonists

DE Uehling, BG Shearer, KH Donaldson…

Index: Uehling, David E.; Shearer, Barry G.; Donaldson, Kelly H.; Chao, Esther Y.; Deaton, David N.; Adkison, Kim K.; Brown, Kathleen K.; Cariello, Neal F.; Faison, Walter L.; Lancaster, Mary E.; Lin, Jasmine; Hart, Robert; Milliken, Tula O.; Paulik, Mark A.; Sherman, Bryan W.; Sugg, Elizabeth E.; Cowan, Conrad Journal of Medicinal Chemistry, 2006 , vol. 49, # 9 p. 2758 - 2771

Full Text: HTML

Citation Number: 30

Abstract

The synthesis of a series of phenethanolamine aniline agonists that contain an aniline ring on the right-hand side of the molecule substituted at the meta position with a benzoic acid or a pyridyl carboxylate is described. Several of the analogues (eg, 34, 36-38, 40, and 44) have high β3 adrenergic receptor (AR) potency and selectivity against β1 and β2 ARs in Chinese hamster ovary (CHO) cells expressing β ARs. The dog pharmacokinetic profile of some of ...