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

  • Sawa M
  • Mizuno K
  • Harada H
 et al. 
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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.

Author-supplied keywords

  • Agonist
  • Tryptamine
  • β3-Adrenergic receptor

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  • Masaaki Sawa

  • Kazuhiro Mizuno

  • Hiroshi Harada

  • Hirotaka Tateishi

  • Yukiyo Arai

  • Shinya Suzuki

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