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Molecules 2011, 16(5), 4104-4121; doi:10.3390/molecules16054104

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

1
Department of Medicinal Chemistry, Jagiellonian University Medical College, 9 Medyczna Street, Kraków 30-688, Poland
2
Équipe Aminoacides Peptides et Protéines, Institut des Biomolécules Max Mousseron IBMM, UMR CNRS 5247, Faculté de Pharmacie, Université Montpellier I et II, 15 avenue Charles Flahault, Montpellier 34060, France
3
Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smętna Street, Kraków 31-343, Poland
4
Department of Chemistry and Chemical Biology, Indiana University-Purdue University Indianapolis, Indianapolis, IN 46202, USA
*
Authors to whom correspondence should be addressed.
Received: 13 April 2011 / Revised: 14 May 2011 / Accepted: 16 May 2011 / Published: 19 May 2011
(This article belongs to the Section Medicinal Chemistry)
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Abstract

We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically active compounds. As an outcome we have synthesized a 24-membered library of arylpiperazine derivatives targeted to 5-HT1A and 5-HT2A receptors. The synthesis was simultaneously performed on BAL-MBHA-PS resin in Poland and the United States, and on BAL-PS-SynPhase Lanterns in France. The D3 project strategy opens the possibility of obtaining potent 5-HT1A/5-HT2A agents in a distributed fashion. While the biological testing is still centralized, this combination of distributed synthesis with screening will enable a D3 network of students world-wide to participate, as part of their education, in the synthesis and testing of this class of biologically active compounds.
Keywords: Distributed Drug Discovery (D3); combinatorial chemistry; solid-phase synthesis; SynPhase Lanterns; long-chain arylpiperazines; succinimides; 5-HT1A; 5-HT2A receptor affinity Distributed Drug Discovery (D3); combinatorial chemistry; solid-phase synthesis; SynPhase Lanterns; long-chain arylpiperazines; succinimides; 5-HT1A; 5-HT2A receptor affinity
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Zajdel, P.; Król, J.; Grychowska, K.; Pawłowski, M.; Subra, G.; Nomezine, G.; Martinez, J.; Satała, G.; Bojarski, A.J.; Zhou, Z.; O’Donnell, M.J.; Scott, W.L. Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents. Molecules 2011, 16, 4104-4121.

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