title: Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists.
abstract: A series of 3-aryl piperidine analogs with 2-piperidinoalkylamino or 2-piperidinoalkyloxy fused bicyclic rings were prepared and found to be potent and efficacious human dopamine D4 agonists. The synthesis and structure-activity relationship (SAR) studies that led to the identification of these compounds are discussed.
authors.affiliation: Neuroscience Research, Global Pharmaceutical Research and Development, AP9A/L16, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. xueqing.wang@abbott.com
authors.forename: Xueqing
authors.initials: X
authors.lastname: Wang
authors.forename: Pramila A
authors.initials: PA
authors.lastname: Bhatia
authors.forename: Jerome F
authors.initials: JF
authors.lastname: Daanen
authors.forename: Steve P
authors.initials: SP
authors.lastname: Latsaw
authors.forename: Jeffrey
authors.initials: J
authors.lastname: Rohde
authors.forename: Teodozyi
authors.initials: T
authors.lastname: Kolasa
authors.forename: Ahmed A
authors.initials: AA
authors.lastname: Hakeem
authors.forename: Mark A
authors.initials: MA
authors.lastname: Matulenko
authors.forename: Masaki
authors.initials: M
authors.lastname: Nakane
authors.forename: Marie E
authors.initials: ME
authors.lastname: Uchic
authors.forename: Loan N
authors.initials: LN
authors.lastname: Miller
authors.forename: Renjie
authors.initials: R
authors.lastname: Chang
authors.forename: Robert B
authors.initials: RB
authors.lastname: Moreland
authors.forename: Jorge D
authors.initials: JD
authors.lastname: Brioni
authors.forename: Andrew O
authors.initials: AO
authors.lastname: Stewart
mesh_terms: D002460:Cell Line; D018491:Dopamine Agonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017448:Receptors, Dopamine D2 / Q000819:agonists*; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
chemical_list: C493599:DRD4 protein, human; D018491:Dopamine Agonists; D008024:Ligands; D010880:Piperidines; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4; C032727:piperidine