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Synthesis and serotonin receptors activity of new purine-2,6-dione derivatives with arylpiperazinylalkoxy moieties |
Grażyna Chłoń-Rzepa 1, Paweł Żmudzki 1, Maciej Pawłowski 1, Andrzej J. Bojarski 2, Beata Duszyńska 2 |
1. Jagiellonian University, Medical College, Department of Pharmaceutical Chemistry, Medyczna 9, Kraków 30-688, Poland |
Abstract |
For several years much attention has been focused on the functional importance of serotonin receptors in the pathogenesis of neuropsychiatric and other diseases. Among many classes of serotonin receptor ligands a long-chain arylpiperazines (LCAPs) containg a different amide/imide terminal fragment were mainly evaluated towards 5-HT1A, 5-HT2A and 5-HT7 receptors. In our earlier studies it was shown that 7-arylalkyl derivatives of 1,3-dimethyl-3,7-dihydropurine-2,6-dione with 8-[3-(4-arylpiperazin-1-yl)-propylamino] moiety, displayed high to moderate affinity for 5-HT1A receptors and moderate to low affinity for 5-HT2A and 5-HT7 sites [1].
The compounds examined in functional in vivo model behaved like postsynaptic 5-HT1A receptor antagonists [1]. To continue our research with this class of purine-2,6-dione analogues we designed and synthesized a novel series of arylpiperazines. Comparing to the previous work structural modifications consisted in replacing the amino group in the 8-position by a ether one.
The new compounds were synthesized in the reaction of previously obtained 1,3-dimethyl-7-arylalkyl-8-bromo-3,7-dihydro-purine-2,6-dione with the appropriate 3-(4-aryl-piperazin-1-yl)-propan-1-ol. The new analogues are under evaluation for their affinity for 5-HT1A, 5-HT2A and 5-HT7 receptors. The most active derivatives will be tested in in vivo behavioral models. [1] G. Chłoń, M. Pawłowski, B. Duszyńska, A. Szaro, E. Tatarczyńska, A. Kłodzińska, E. Chojnacka-Wójcik: Pol. J. Pharmacol., 2001, 53, 359-368. |
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Presentation: Poster at VI Multidyscyplinarna Konferencja Nauki o Leku, by Grażyna Chłoń-RzepaSee On-line Journal of VI Multidyscyplinarna Konferencja Nauki o Leku Submitted: 2008-03-10 15:03 Revised: 2009-06-07 00:48 |