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Title: Search for new adenosine receptor ligands and MAO-B inhibitors in a group of xanthine derivatives
Abstract:
The aim of this thesis was to conduct studies on the multidirectional activity of xanthine derivatives, including an attempt to describe which structural elements determine the activity towards adenosine receptor subtypes or the MAO-B inhibitory activity. In the dissertation, a series of new compounds were developed, which through their multi-target mechanism of action may in the future be an alternative to the currently used therapy of neurodegenerative diseases. In addition, a series of selective A2B adenosine receptor antagonists were developed during the stay at the Rhine University in Bonn. A series of modifications leading to new structures included changes within positions: N1, N3, N7 and C8 of the xanthine core. These modifications were caused by the desire to determine the structural elements important for selectivity and activity towards A1, A2A, A2B receptors and MAO-B enzyme. 165 new compounds were developed - 135 in the series of multifunctional ligands and 30 in the group of A2B adenosine receptor antagonists. The result of the work was the obtaining of compounds that, as a result of their multidirectional activity, can be considered in the future as lead structures for further research. In addition, SAR analysis of the developed ligands are a source of information, facilitating the development of research on structures combining A1/A2A and MAO-B activity to o ; btain multifunctional compounds. Another result was the introduction and optimization of methods for the synthesis of selected structures using microwaves, whereby solvent consumption was reduced, reaction time was shortened or yields were raised compared to literature methods.
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Rada Dyscypliny Nauki farmaceutyczne
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Last modified:
Apr 8, 2024
In our library since:
Apr 8, 2024
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http://dl.cm-uj.krakow.pl:8080/publication/5066
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| Edition name | Date |
|---|---|
| ZB-139423 | Apr 8, 2024 |
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