title: Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.
abstract: A series of tryptamine-based 2-thiophenesulfonamide derivatives were prepared and their agonistic activity for the beta-adrenergic receptors (ARs) was evaluated. Compound 54, containing 7-methanesulfonyloxy tryptamine, was found to be a highly potent beta3-AR agonist (EC50=0.21 nM, IA=97%) with excellent selectivity for the beta3-AR over the beta1- and beta2-ARs (210- and 86-fold, respectively).
authors.affiliation: Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd, 33-94, Enoki, Suita 564-0053, Japan. kazuhiro-mizuno@dainippon-pharm.co.jp
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Mizuno
authors.forename: Masaaki
authors.initials: M
authors.lastname: Sawa
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Harada
authors.forename: Hirotaka
authors.initials: H
authors.lastname: Tateishi
authors.forename: Mayumi
authors.initials: M
authors.lastname: Oue
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tsujiuchi
authors.forename: Yasuji
authors.initials: Y
authors.lastname: Furutani
authors.forename: Shiro
authors.initials: S
authors.lastname: Kato
mesh_terms: D058665:Adrenergic beta-1 Receptor Agonists; D058666:Adrenergic beta-2 Receptor Agonists; D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry; D014363:Tryptamines / Q000737:chemistry*
chemical_list: D058665:Adrenergic beta-1 Receptor Agonists; D058666:Adrenergic beta-2 Receptor Agonists; D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D007211:Indoles; D013449:Sulfonamides; D013876:Thiophenes; D014363:Tryptamines