A Solution-Phase Combinatorial Synthesis of Selective Dopamine D4 Ligands

Title: A Solution-Phase Combinatorial Synthesis of Selective Dopamine D4 Ligands

Volume: 3 Issue: 1

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

Affiliation:

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

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

Cite this article as:

Williams P. John and Lavrador Karine, A Solution-Phase Combinatorial Synthesis of Selective Dopamine D4 Ligands, Combinatorial Chemistry & High Throughput Screening 2000; 3 (1) . https://dx.doi.org/10.2174/1386207003327710