Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety

The continued SAR investigation of tryptamine-based human beta(3)-adrenergic receptor (AR) agonists is reported. Prior efforts resulted in the identification of 2 as a potent beta(3)-AR agonist. Further modification of the left side arylsulfonamide portion in 2 provided compounds with good cell perm...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (4), p.1061
Hauptverfasser:	Sawa, Masaaki, Mizuno, Kazuhiro, Harada, Hiroshi, Tateishi, Hirotaka, Arai, Yukiyo, Suzuki, Shinya, Oue, Mayumi, Tsujiuchi, Hiroshi, Furutani, Yasuji, Kato, Shiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Adrenergic Agonists - chemical synthesis Adrenergic Agonists - pharmacokinetics Adrenergic Agonists - pharmacology Biological Availability Cell Membrane Permeability Humans Inhibitory Concentration 50 Receptors, Adrenergic, beta-3 - metabolism Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - pharmacokinetics Sulfonamides - pharmacology Tryptamines
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Zusammenfassung:	The continued SAR investigation of tryptamine-based human beta(3)-adrenergic receptor (AR) agonists is reported. Prior efforts resulted in the identification of 2 as a potent beta(3)-AR agonist. Further modification of the left side arylsulfonamide portion in 2 provided compounds with good cell permeability, which have potent agonistic activity for beta(3)-AR. Cinnamylamine analog 16i exhibited an excellent agonistic profile in vitro and good oral bioavailability in rats.
ISSN:	0960-894X