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Evaluation of a novel series of [1,2,4] triazolo [4,3-a] quinoxalines and related compounds: highly potent adenosine receptor antagonists
Krpelíková, Irena ; Vopršalová, Marie (advisor) ; Macháček, Miloš (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmacology and Toxicology, Czech Republic Performed at: University of Bonn, Pharmaceutical Institute, Department of Pharmaceutical Chemistry, Germany Candidate: Irena Krpelíková Supervisors: Prof. Dr. Christa Elisabeth Müller PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: Evaluation of a novel series of [1,2,4]triazolo[4,3- ɑ]quinoxalines and related compounds: highly potent adenosine receptor antagonists Adenosine, a local modulator, acts in many diverse biological processes. Its effects are mediated through adenosine receptors (ARs). Four types of ARs have been described, A1, A2A, A2B and A3, which belong to the superfamily of G protein-coupled receptors. AR ligands are being developed as new drugs. This thesis deals with the study of a novel series of [1,2,4]triazolo[4,3- a]quinoxalines and related compounds as potential adenosine receptor antagonists. The presented results were obtained using radioligand binding assays. Series of quinoxalinones and tetrazoloquinoxalines exhibit significant selectivity for human (h) A3 ARs but their affinity is relatively low for tetrazoloquinoxalines and moderate for quinoxalinones. Triazoloquinoxalines comprise the largest group of this series. Generally, the R1...
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