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A Solution-Phase Combinatorial Synthesis of Selective Dopamine D4 Ligands

[ Vol. 3 , Issue. 1 ]


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


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


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


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

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