Title of article
Synthesis and functional activity of (2-aryl-1-piperazinyl)-N-(3-methylphenyl)acetamides: selective dopamine D4 receptor agonists Original Research Article
Author/Authors
Mark A. Matulenko، نويسنده , , Ahmed A Hakeem، نويسنده , , Teodozyi Kolasa، نويسنده , , Masaki Nakane، نويسنده , , Marc A. Terranova، نويسنده , , Marie E. Uchic، نويسنده , , Loan N. Miller، نويسنده , , Renjie Chang، نويسنده , , Diana L. Donnelly-Roberts، نويسنده , , Marian T. Namovic، نويسنده , , Robert B. Moreland، نويسنده , , Jorge D. Brioni، نويسنده , , Andrew O Stewart، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
13
From page
3471
To page
3483
Abstract
Diaryl piperazine acetamides were identified as potent and selective dopamine D4 receptor agonists. Our strategy is based on an amide bond reversal of an acid sensitive, dopamine D4 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 D4 agonists is discussed.
Keywords
Dopamine , D4 receptor , Agonists , Piperazine
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2004
Journal title
Bioorganic and Medicinal Chemistry
Record number
1303148
Link To Document