Abstract
The continued SAR investigation of tryptamine-based human β3-adrenergic receptor (AR) agonists is reported. Prior efforts resulted in the identification of 2 as a potent β3-AR agonist. Further modification of the left side arylsulfonamide portion in 2 provided compounds with good cell permeability, which have potent agonistic activity for β3-AR. Cinnamylamine analog 16i exhibited an excellent agonistic profile in vitro and good oral bioavailability in rats. © 2004 Elsevier Ltd. All rights reserved.
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Sawa, M., Mizuno, K., Harada, H., Tateishi, H., Arai, Y., Suzuki, S., … Kato, S. (2005). Tryptamine-based human β3-adrenergic receptor agonists. Part 3: Improved oral bioavailability via modification of the sulfonamide moiety. Bioorganic and Medicinal Chemistry Letters, 15(4), 1061–1064. https://doi.org/10.1016/j.bmcl.2004.12.033
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