title: Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
abstract: We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. shuwen_he@merck.com
authors.forename: Shuwen
authors.initials: S
authors.lastname: He
authors.forename: Peter H
authors.initials: PH
authors.lastname: Dobbelaar
authors.forename: Jian
authors.initials: J
authors.lastname: Liu
authors.forename: Tianying
authors.initials: T
authors.lastname: Jian
authors.forename: Iyassu K
authors.initials: IK
authors.lastname: Sebhat
authors.forename: Linus S
authors.initials: LS
authors.lastname: Lin
authors.forename: Allan
authors.initials: A
authors.lastname: Goodman
authors.forename: Cheng
authors.initials: C
authors.lastname: Guo
authors.forename: Peter R
authors.initials: PR
authors.lastname: Guzzo
authors.forename: Mark
authors.initials: M
authors.lastname: Hadden
authors.forename: Alan J
authors.initials: AJ
authors.lastname: Henderson
authors.forename: Megan
authors.initials: M
authors.lastname: Ruenz
authors.forename: Bruce J
authors.initials: BJ
authors.lastname: Sargent
authors.forename: Larry
authors.initials: L
authors.lastname: Yet
authors.forename: Theresa M
authors.initials: TM
authors.lastname: Kelly
authors.forename: Oksana
authors.initials: O
authors.lastname: Palyha
authors.forename: Yanqing
authors.initials: Y
authors.lastname: Kan
authors.forename: Jie
authors.initials: J
authors.lastname: Pan
authors.forename: Howard
authors.initials: H
authors.lastname: Chen
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Marsh
authors.forename: Lauren P
authors.initials: LP
authors.lastname: Shearman
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Joseph M
authors.initials: JM
authors.lastname: Metzger
authors.forename: Scott D
authors.initials: SD
authors.lastname: Feighner
authors.forename: Carina
authors.initials: C
authors.lastname: Tan
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Howard
authors.forename: Constantin
authors.initials: C
authors.lastname: Tamvakopoulos
authors.forename: Qianping
authors.initials: Q
authors.lastname: Peng
authors.forename: Xiao-Ming
authors.initials: XM
authors.lastname: Guan
authors.forename: Marc L
authors.initials: ML
authors.lastname: Reitman
authors.forename: Arthur A
authors.initials: AA
authors.lastname: Patchett
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
mesh_terms: D000818:Animals; D001682:Biological Availability; D055808:Drug Discovery; D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D018004:Receptors, Bombesin / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D007093:Imidazoles; D018004:Receptors, Bombesin; C107120:bombesin receptor subtype 3