Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists.
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.
Wang
Xueqing
X
Neuroscience Research, Global Pharmaceutical Research and Development, AP9A/L16, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. xueqing.wang@abbott.com
Bhatia
Pramila A
PA
Daanen
Jerome F
JF
Latsaw
Steve P
SP
Rohde
Jeffrey
J
Kolasa
Teodozyi
T
Hakeem
Ahmed A
AA
Matulenko
Mark A
MA
Nakane
Masaki
M
Uchic
Marie E
ME
Miller
Loan N
LN
Chang
Renjie
R
Moreland
Robert B
RB
Brioni
Jorge D
JD
Stewart
Andrew O
AO
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
C493599:DRD4 protein, human; D018491:Dopamine Agonists; D008024:Ligands; D010880:Piperidines; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4; C032727:piperidine