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Title: Synthesis and chemical-pharmacological studies of new derivatives 1,3-substituted pyrrolidine-2,5-dione with potential anticonvulsant activity
Abstract:
The aim of the dissertation was to obtain new 1,3-substituted-pyrrolidine-2,5-dione derivatives. The main structural modifications concerned the substituent at the 3-position of pyrrolidine-2,5-dione ring, the linker between this system and the variously substituted arylpiperazine, and the replacement of arylpiperazine with morpholine in order to assess the effect of these changes on anticonvulsant activity. In the experimental part, a multi-step synthesis was described, as a result of which fifty-one compounds were obtained, which were tested for anticonvulsant activity at the Department of Pharmacodynamics, UJ CM. The obtained results showed that sixteen of the tested compounds showed anticonvulsant activity, mainly in the 6 Hz test, some also in the MES test. Then, quantitative tests were performed for these compounds, the most active compound was 2g 3-(benzo [b] thiophen-2-yl)-1-(2-morpholinopropyl)-pyrrolidine-2,5-dione. Nine selected compounds were also tested for analgesic activity. The most active compounds were 3a - 3-benzhydryl-1-{2-[4-(3-trifluoromethylphenyl)piperazin-1-yl]-2-oxoethyl}-pyrrolidine-2,5-dione, and 7f – 1-3-[4- (3,4-dichlorophenyl)piperazin-1-yl]propyl}-3-(3-methylthiophen-2-yl)-pyrrolidine-2,5-dione hydrochloride. For selected active compounds, in vitro affinity tests for sodium and calcium channels, GABAA and TRPV1 receptors, GABA transporters, an ; d the assessment of hepatotoxic properties in the PrestoBlue test and physicochemical properties based on the rules of Lipiński and Veber (SwissAdme) were performed.
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Rada Dyscypliny Nauki farmaceutyczne
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Obniska, Jolanta ; Czopek, Anna
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Last modified:
Mar 25, 2024
In our library since:
Mar 31, 2022
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http://dl.cm-uj.krakow.pl:8080/publication/4603
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| Edition name | Date |
|---|---|
| ZB-133522 | Mar 25, 2024 |
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