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Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides
L L Brockunier1, E R Parmee, H O Ok
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. linda_brockunier@merck.com
Bioorganic & Medicinal Chemistry Letters
|September 22, 2000
Abstract:
Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were prepared and found to be potent and selective human beta3-adrenergic receptor agonists. The most interesting compound, trifluoromethylbenzyl analogue 12e (beta3 EC50 = 3.1 nM with >1500-fold selectivity over binding to both beta1- and beta2 receptors), stimulates lipolysis in the rhesus monkey (ED50 = 0.36 mg/kg) and is 25% orally bioavailable in the dog.