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Title: Novel anilide and benzylamide derivatives as 5-HT1A/5- HT7 receptor ligands and phosphodiesterase type 4 and 7 inhibitors with potential procognitive and antidepressant activity


The search for drugs for the treatment of memory and mood disorders belongs to one of the leading research topics worldwide. The aim of the thesis was to design and synthesize novel anilide and benzylamide derivatives of long-chain cyclic amines as multifunctional ligands of serotonin 5-HT1A and 5-HT7 receptors as well as phosphodiesterase (POE) 4 and 7 inhibitors with potentia! procognitive and antidepressant properties. A series of 90 designed compounds was obtained by using classical organie chemistry methods. The synthesized derivatives were potent-to-weak 5-HT1A and 5-HT7 receptors ligands. Many of them showed features of PDE4B and/or PDE7A inhibitors. On the basis of the obtained in vitro results, structure- activity relationship studies were performed. In vitro functional tests enabled to select potent 5-HT1A receptor antagonists with various 5-HT7 receptor antagonistic properties. In vitro ADME studies allowed to select high-permeable compounds with improved metabolic stability. The most promising derivatives showed procognitive and antidepressant properties in vivo. Finally, neuroprotective properties in vitro were demonstrated for the representative compounds. Research results suggest that the simultaneous interaction with 5- HT 1A and 5-HT7 receptors and PDE4B and/or PDE7A inhibition may be a promising strategy for treating cognitive and depressive disorders.

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2 - studia doktoranckie

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Rada Dyscypliny Nauki farmaceutyczne


Chłoń-Rzepa, Grażyna

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eng; pol

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tylko w bibliotece

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Last modified:

Apr 30, 2024

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Mar 31, 2022

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ZB-134218 Apr 30, 2024


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