title: Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family.
abstract: The synthesis and muscarinic binding properties of compounds based on the 1-[4-(4-arylsulfonyl)phenylmethyl]-4-(1-aroyl-4-piperidinyl)-piperazine skeleton are described. For compounds, substituted with appropriately configured methyl groups at the benzylic center and at the piperazine 2-position, high levels of selective, M(2) subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.
authors.affiliation: Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. stuart.mccombie@spcorp.com
authors.forename: Stuart W
authors.initials: SW
authors.lastname: McCombie
authors.forename: Sue Ing
authors.initials: SI
authors.lastname: Lin
authors.forename: Jayaram R
authors.initials: JR
authors.lastname: Tagat
authors.forename: Dennis
authors.initials: D
authors.lastname: Nazareno
authors.forename: Susan
authors.initials: S
authors.lastname: Vice
authors.forename: Jennifer
authors.initials: J
authors.lastname: Ford
authors.forename: Theodros
authors.initials: T
authors.lastname: Asberom
authors.forename: Daria
authors.initials: D
authors.lastname: Leone
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Kozlowski
authors.forename: Guowei
authors.initials: G
authors.lastname: Zhou
authors.forename: Vilma B
authors.initials: VB
authors.lastname: Ruperto
authors.forename: Ruth A
authors.initials: RA
authors.lastname: Duffy
authors.forename: Jean E
authors.initials: JE
authors.lastname: Lachowicz
mesh_terms: D001665:Binding Sites; D008024:Ligands; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D010879:Piperazines; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic