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Title: Tricyclic theophylline derivatives with arylalkylpiperazinyl moiety as CNS receptor' ligands
Abstract:
The presented work is a part of research on tricyclic theophylline derivatives, conduct m Departament of Medicinal Chemistry Jagiellonian University Medical College. In the introduction mechanism of action and possibilities of therapeutical use of theophylline and its derivatives were described, pat1icularly effects on adenosine receptors, phosphodiesterases and localization and transp011 of calcium ions was discussed. Development of research on tricyclic derivativ~s of 7H-purine was also presented. In the experimental part, the synthesis of arylalkilpiperazinyl derivatives of imidazo[2, 1-f]theophylline was presented. The modifications of lead structure were made at 7 position (methyl or phenyl substituent); at alkilene spacer between imidazo[2, 1- f]theophylline and arylpiperazinyl moiety, and also at phenyl ring at arylpiperazinyl moiety. For all compounds the logP parameter was detennined. The affinity for CNS receptors was investigated (5-HT1A, 5-HT2A i D2) and for the selected compounds, anxiolytic and antidepressant activity was evaluated. Furthennore, the interaction between arylalkilpiperazinyl derivatives of imidazo[2,1- f]theophylline and the 5-HT1A receptor was analyzed by simulated docking to the 5-HT1A receptor model. Moreover the Free-Wilson and Fujita-Ban QSAR analysis was also realized. The results of described studies indicated that ; the tricyclic theophylline derivatives are interesting new CNS receptor' ligands.
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Last modified:
Jan 30, 2023
In our library since:
Nov 21, 2012
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35
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0
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http://dl.cm-uj.krakow.pl:8080/publication/988
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| Edition name | Date |
|---|---|
| ZB-107455 | Jan 30, 2023 |
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