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ID: ALA1138712

Journal: Bioorg Med Chem Lett

Title: Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.

Authors: Mizuno K, Sawa M, Harada H, Tateishi H, Oue M, Tsujiuchi H, Furutani Y, Kato S.

Abstract: A series of tryptamine-based 2-thiophenesulfonamide derivatives were prepared and their agonistic activity for the beta-adrenergic receptors (ARs) was evaluated. Compound 54, containing 7-methanesulfonyloxy tryptamine, was found to be a highly potent beta3-AR agonist (EC50=0.21 nM, IA=97%) with excellent selectivity for the beta3-AR over the beta1- and beta2-ARs (210- and 86-fold, respectively).

CiteXplore: 15546707

DOI: 10.1016/j.bmcl.2004.10.035