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Bioorg Med Chem. 2004 Jul 1;12(13):3471-83.

Synthesis and functional activity of (2-aryl-1-piperazinyl)-N-(3-methylphenyl)acetamides: selective dopamine D4 receptor agonists.

Author information

1
Neuroscience Research, Global Pharmaceutical Research, Abbott Laboratories, Abbott Park, IL 60064, USA. mark.a.matulenko@abbott.com

Abstract

Diaryl piperazine acetamides were identified as potent and selective dopamine D(4) receptor agonists. Our strategy is based on an amide bond reversal of an acid sensitive, dopamine D(4) receptor partial agonist, PD 168077. This reversal provided compounds with excellent potency and improved stability. Systematic evaluation of the substitution on the aryl piperazine portion revealed a significant effect on functional activity. The synthesis and biological activity of these new dopamine D(4) agonists is discussed.

PMID:
15186832
DOI:
10.1016/j.bmc.2004.04.035
[Indexed for MEDLINE]

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