title: Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
abstract: A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatment of overactive bladder.
authors.affiliation: Merck Research Laboratories, Rahway, NJ 07065, USA. stephen_goble@merck.com
authors.forename: Stephen D
authors.initials: SD
authors.lastname: Goble
authors.forename: Liping
authors.initials: L
authors.lastname: Wang
authors.forename: K Lulu
authors.initials: KL
authors.lastname: Howell
authors.forename: Alka
authors.initials: A
authors.lastname: Bansal
authors.forename: Richard
authors.initials: R
authors.lastname: Berger
authors.forename: Linda
authors.initials: L
authors.lastname: Brockunier
authors.forename: Jerry
authors.initials: J
authors.lastname: DiSalvo
authors.forename: Scott
authors.initials: S
authors.lastname: Feighner
authors.forename: Bart
authors.initials: B
authors.lastname: Harper
authors.forename: Jiafang
authors.initials: J
authors.lastname: He
authors.forename: Amanda
authors.initials: A
authors.lastname: Hurley
authors.forename: Donna
authors.initials: D
authors.lastname: Hreniuk
authors.forename: Emma
authors.initials: E
authors.lastname: Parmee
authors.forename: Michael
authors.initials: M
authors.lastname: Robbins
authors.forename: Gino
authors.initials: G
authors.lastname: Salituro
authors.forename: Anthony
authors.initials: A
authors.lastname: Sanfiz
authors.forename: Eric
authors.initials: E
authors.lastname: Streckfuss
authors.forename: Eloisa
authors.initials: E
authors.lastname: Watkins
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
authors.forename: Mary
authors.initials: M
authors.lastname: Struthers
authors.forename: Scott D
authors.initials: SD
authors.lastname: Edmondson
mesh_terms: D000081:Acetamides / Q000493:pharmacokinetics / Q000494:pharmacology*; D058667:Adrenergic beta-3 Receptor Agonists; D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001549:Benzamides / Q000493:pharmacokinetics / Q000494:pharmacology*; D012377:Rodentia; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D058667:Adrenergic beta-3 Receptor Agonists; D000319:Adrenergic beta-Antagonists; D001549:Benzamides