884331-11-7Relevant articles and documents
Tryptamine-based human β3-adrenergic receptor agonists. Part 3: Improved oral bioavailability via modification of the sulfonamide moiety
Sawa, Masaaki,Mizuno, Kazuhiro,Harada, Hiroshi,Tateishi, Hirotaka,Arai, Yukiyo,Suzuki, Shinya,Oue, Mayumi,Tsujiuchi, Hiroshi,Furutani, Yasuji,Kato, Shiro
, p. 1061 - 1064 (2007/10/03)
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.