title: The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.
abstract: A structure-activity relationship study of the lead piperazinylcarbonylpiperidine compound 3 resulted in the identification of 4-benzimidazolyl-piperidinylcarbonyl-piperidine 6h as a histamine-3 (H(3)) receptor antagonist. Additional optimization of 6h led to the identification of compounds 11i-k with K(i) <or= 0.5 nM and good in vivo activity.
authors.affiliation: Department of Chemical Research, Merck Research Laboratories, Kenilworth, NJ 07033, USA. pauline.ting@merck.com
authors.forename: Pauline C
authors.initials: PC
authors.lastname: Ting
authors.forename: Joe F
authors.initials: JF
authors.lastname: Lee
authors.forename: Margaret M
authors.initials: MM
authors.lastname: Albanese
authors.forename: Jie
authors.initials: J
authors.lastname: Wu
authors.forename: Robert
authors.initials: R
authors.lastname: Aslanian
authors.forename: Leonard
authors.initials: L
authors.lastname: Favreau
authors.forename: Cymbelene
authors.initials: C
authors.lastname: Nardo
authors.forename: Walter A
authors.initials: WA
authors.lastname: Korfmacher
authors.forename: Robert E
authors.initials: RE
authors.lastname: West
authors.forename: Shirley M
authors.initials: SM
authors.lastname: Williams
authors.forename: John C
authors.initials: JC
authors.lastname: Anthes
authors.forename: Maria A
authors.initials: MA
authors.lastname: Rivelli
authors.forename: Michel R
authors.initials: MR
authors.lastname: Corboz
authors.forename: John A
authors.initials: JA
authors.lastname: Hey
mesh_terms: D054828:Histamine H3 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D054828:Histamine H3 Antagonists; D010880:Piperidines