Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists

Xueqing Wang; Pramila A Bhatia; Jerome F Daanen; Steve P Latsaw; Jeffrey Rohde; Teodozyi Kolasa; Ahmed A Hakeem; Mark A Matulenko; Masaki Nakane; Marie E Uchic; Loan N Miller; Renjie Chang; Robert B Moreland; Jorge D Brioni; Andrew O Stewart

doi:10.1016/j.bmc.2005.04.060

Synthesis and evaluation of 3-aryl piperidine analogs as potent and efficacious dopamine D4 receptor agonists

Bioorg Med Chem. 2005 Aug 1;13(15):4667-78. doi: 10.1016/j.bmc.2005.04.060.

Authors

Xueqing Wang¹, Pramila A Bhatia, Jerome F Daanen, Steve P Latsaw, Jeffrey Rohde, Teodozyi Kolasa, Ahmed A Hakeem, Mark A Matulenko, Masaki Nakane, Marie E Uchic, Loan N Miller, Renjie Chang, Robert B Moreland, Jorge D Brioni, Andrew O Stewart

Affiliation

¹ Neuroscience Research, Global Pharmaceutical Research and Development, AP9A/L16, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. [email protected]

PMID: 15896964
DOI: 10.1016/j.bmc.2005.04.060

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.

MeSH terms

Cell Line
Dopamine Agonists / chemical synthesis*
Dopamine Agonists / chemistry
Dopamine Agonists / pharmacology*
Humans
Ligands
Molecular Structure
Piperidines / chemical synthesis
Piperidines / chemistry*
Piperidines / pharmacology*
Receptors, Dopamine D2 / agonists*
Receptors, Dopamine D4
Structure-Activity Relationship

Substances

DRD4 protein, human
Dopamine Agonists
Ligands
Piperidines
Receptors, Dopamine D2
Receptors, Dopamine D4
piperidine