title: Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
abstract: We report the discovery of novel histamine H(3) receptor antagonists based on 4-[(1H-imidazol-4-yl)methyl]piperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.
authors.affiliation: The Schering Plough Research Institute, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
authors.forename: Wayne D
authors.initials: WD
authors.lastname: Vaccaro
authors.forename: Rosy
authors.initials: R
authors.lastname: Sher
authors.forename: Michael
authors.initials: M
authors.lastname: Berlin
authors.forename: Neng-Yang
authors.initials: NY
authors.lastname: Shih
authors.forename: Robert
authors.initials: R
authors.lastname: Aslanian
authors.forename: John H
authors.initials: JH
authors.lastname: Schwerdt
authors.forename: Kevin D
authors.initials: KD
authors.lastname: McCormick
authors.forename: John J
authors.initials: JJ
authors.lastname: Piwinski
authors.forename: Robert E
authors.initials: RE
authors.lastname: West
authors.forename: John C
authors.initials: JC
authors.lastname: Anthes
authors.forename: Shirley M
authors.initials: SM
authors.lastname: Williams
authors.forename: Ren-Long
authors.initials: RL
authors.lastname: Wu
authors.forename: H Susan
authors.initials: HS
authors.lastname: She
authors.forename: Maria A
authors.initials: MA
authors.lastname: Rivelli
authors.forename: Jennifer C
authors.initials: JC
authors.lastname: Mutter
authors.forename: Michel R
authors.initials: MR
authors.lastname: Corboz
authors.forename: John A
authors.initials: JA
authors.lastname: Hey
authors.forename: Leonard
authors.initials: L
authors.lastname: Favreau
mesh_terms: D065690:Cytochrome P-450 CYP2D6 Inhibitors; D004353:Drug Evaluation, Preclinical; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D065690:Cytochrome P-450 CYP2D6 Inhibitors; D006633:Histamine Antagonists; D007093:Imidazoles; D010880:Piperidines; D018100:Receptors, Histamine H3; C085755:4-(1H-imidazol-4-ylmethyl)piperidine