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ID: ALA1133315

Journal: Bioorg Med Chem Lett

Title: Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Authors: Brockunier LL, Parmee ER, Ok HO, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

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.

CiteXplore: 10999482

DOI: 10.1016/s0960-894x(00)00422-4