Author/Authors :
Masaaki Sawa، نويسنده , , Kazuhiro Mizuno، نويسنده , , Hiroshi Harada، نويسنده , , Hirotaka Tateishi، نويسنده , , Yukiyo Arai، نويسنده , , Shinya Suzuki، نويسنده , , Mayumi Oue، نويسنده , , Hiroshi Tsujiuchi، نويسنده , , Yasuji Furutani، نويسنده , , Shiro Kato، نويسنده ,
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.
