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ID: ALA1132774
Journal: Bioorg Med Chem Lett
Title: Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
Authors: Parmee ER, Brockunier LL, He J, Singh SB, Candelore MR, Cascieri MA, Deng L, Liu Y, Tota L, Wyvratt MJ, Fisher MH, Weber AE.
Abstract: Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta3 AR. Naphthyloxy compound 18 (beta3 EC50 = 78 nM) did not activate the beta1 and beta2 ARs at 10 microM, and showed >1000-fold selectivity over binding to the beta1 and beta2 ARs.
CiteXplore: 11055339