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A Solution-Phase Combinatorial Synthesis of Selective Dopamine D4 Ligands

[ Vol. 3 , Issue. 1 ]

Author(s):

John P. Williams and Karine Lavrador   Pages 43 - 50 ( 8 )

Abstract:


Utilizing combinatorial synthesis and a preparative LC-MS automated chromatography system we have prepared and purified a library of 4-(2-(1,2,4-oxadiazolyl)piperidines that were designed to be novel and selective dopamine D4 ligands. In one round of synthesis we identified N-4-chlorobenzyl-4-(2-(3-(2-thienyl)-1,2,4-oxadiazolyl))piperidine with a Kd of 5 nM for the human D4 receptor

Keywords:

Solution phase combinatorial synthesis, Selective dopamine D4 Ligands, Coat protein, Ligand design, D4 antagonists, Clozapine, Chlorpromazine, Neuroleptics, Haloperidol

Affiliation:

Department of Medicinal Chemistry, CombiChem, Inc. San Diego, CA 92121, USA



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