Tryptamine-based human β3-adrenergic receptor agonists. Part 3: Improved oral bioavailability via modification of the sulfonamide moiety

A series of tryptamine-based human β3-adrenergic receptor (AR) agonists were synthesized in an effort to improve oral bioavailability. Cinnamylamine analog 16i exhibited an excellent agonistic profile in vitro and good oral bioavailability in rats.