title: BMS-201620: a selective beta 3 agonist.
abstract: A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA. william.washburn@bms.com
authors.forename: W N
authors.initials: WN
authors.lastname: Washburn
authors.forename: C-Q
authors.initials: CQ
authors.lastname: Sun
authors.forename: G
authors.initials: G
authors.lastname: Bisacchi
authors.forename: G
authors.initials: G
authors.lastname: Wu
authors.forename: P T
authors.initials: PT
authors.lastname: Cheng
authors.forename: P M
authors.initials: PM
authors.lastname: Sher
authors.forename: D
authors.initials: D
authors.lastname: Ryono
authors.forename: A V
authors.initials: AV
authors.lastname: Gavai
authors.forename: K
authors.initials: K
authors.lastname: Poss
authors.forename: R N
authors.initials: RN
authors.lastname: Girotra
authors.forename: P J
authors.initials: PJ
authors.lastname: McCann
authors.forename: A B
authors.initials: AB
authors.lastname: Mikkilineni
authors.forename: T C
authors.initials: TC
authors.lastname: Dejneka
authors.forename: T C
authors.initials: TC
authors.lastname: Wang
authors.forename: Z
authors.initials: Z
authors.lastname: Merchant
authors.forename: M
authors.initials: M
authors.lastname: Morella
authors.forename: C M
authors.initials: CM
authors.lastname: Arbeeny
authors.forename: T W
authors.initials: TW
authors.lastname: Harper
authors.forename: D A
authors.initials: DA
authors.lastname: Slusarchyk
authors.forename: S
authors.initials: S
authors.lastname: Skwish
authors.forename: A D
authors.initials: AD
authors.lastname: Russell
authors.forename: G T
authors.initials: GT
authors.lastname: Allen
authors.forename: B
authors.initials: B
authors.lastname: Tesfamariam
authors.forename: B H
authors.initials: BH
authors.lastname: Frohlich
authors.forename: B E
authors.initials: BE
authors.lastname: Abboa-Offei
authors.forename: M
authors.initials: M
authors.lastname: Cap
authors.forename: T L
authors.initials: TL
authors.lastname: Waldron
authors.forename: R J
authors.initials: RJ
authors.lastname: George
authors.forename: D
authors.initials: D
authors.lastname: Young
authors.forename: K E
authors.initials: KE
authors.lastname: Dickinson
authors.forename: A A
authors.initials: AA
authors.lastname: Seymour
mesh_terms: D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000882:Haplorhini; D006801:Humans; D008745:Methylation; D022702:Receptors, Adrenergic, beta-3 / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; C495735:BMS-201620; D022702:Receptors, Adrenergic, beta-3; C018556:glycine amide; D005998:Glycine