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Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties
L L Brockunier1, M R Candelore, M A Cascieri
1Department of Medicinal Chemistry, Biochemistry and Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorganic & Medicinal Chemistry Letters
|February 24, 2001
Abstract:
Pyridineethanolamine derivatives containing cyanoguanidine or nitroethylenediamine moieties were examined as human beta3 adrenergic receptor (AR) agonists. Notably, indoline derivatives 6a and 11 were potent beta3 AR agonists (beta3 EC50 = 13 and 19 nM, respectively), which showed good selectivity over binding to and minimal activation of the beta1 and beta2 ARs.