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Synthesis of novel pyrido[1,2-c]pyrimidine derivatives as selective ligands for 5-HT1A receptors
|Franciszek Herold 1, Agnieszka Ciesielska 2, Andrzej J. Bojarski 3, Gabriel Nowak 4
1. Medical University of Warsaw, Department of Drug Technology, Banacha 1a, Warszawa 02-097, 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.
Presentation: Poster at VI Multidyscyplinarna Konferencja Nauki o Leku, by Agnieszka Ciesielska
See On-line Journal of VI Multidyscyplinarna Konferencja Nauki o Leku
Submitted: 2008-03-12 21:49 Revised: 2009-06-07 00:48