| Literature DB >> 10999482 |
L L Brockunier1, E R Parmee, H O Ok, M R Candelore, M A Cascieri, L F Colwell, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, L Tota, M J Wyvratt, M H Fisher, A E Weber.
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.Entities:
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Year: 2000 PMID： 10999482 DOI： 10.1016/s0960-894x(00)00422-4
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823