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Synthesis of novel pyrido[1,2-c]pyrimidine derivatives as selective ligands for 5-HT1A receptors

Franciszek Herold 1Agnieszka Ciesielska 2Andrzej J. Bojarski 3Gabriel Nowak 4

1. Medical University of Warsaw, Department of Drug Technology, Banacha 1a, Warszawa 02-097, Poland
2. Pharmaceutical Research Institute (IF), Rydygiera 8, Warszawa 01-793, Poland
3. Polish Academy of Sciences. Institute of Pharmacology, Smętna 12, Kraków 31-343, Poland
4. Jagiellonian University Collegium Medicum, Department of Pharmacodynamics (JUCM), Medyczna 9, Kraków 30-688, Poland


Serotonin (5-HT) is an important neurotransmitter mediator in the peripheral and central nervous system. Serotonin 5-HT1A receptors have been intensively studied because of their implication in several physiological processes and psychiatric disorders such as anxiety and depression. 5-HT1A receptor ligands with serotonin transporter inhibition effect are regarded as potential therapeutics for anxiety, depression. Moreover the chemical structure of synthesized ligands may be responsible for pre- and post-synapsis agonism or antagonism effect on 5-HT1A receptors.

Although the main investigated structures were buspirone and tandospirone, many modifications have been made in the pharmacophoric and non-pharmacophoric part of potential 5-HT1A receptors ligands.

All novel 4-aryl-2H-pyrido[1,2-c]pyrimidine derivatives containing quinoline substituents were confirmed by1H and 13C NMR spectra and elementar analysis. Target compounds were assesed for in vitro affinity for serotoninergic 5-HT1A and 5-HT2A receptors and 5-HT-T.


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Submitted: 2008-03-12 21:49
Revised:   2009-06-07 00:48