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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

A Solution-Phase Combinatorial Synthesis of Selective Dopamine D4 Ligands

Author(s): John P. Williams and Karine Lavrador

Volume 3, Issue 1, 2000

Page: [43 - 50] Pages: 8

DOI: 10.2174/1386207003327710

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


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