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Title: Chemical and pharmacological studies in group of 3,3-disubstituted derivatives of pyrrolidyne-2,5-dion with potential anticonvulsant activity
Abstract:
This thesis presents the search for new active anticonvulsant compounds in group of 3,3-disubstituted pyrrolidyne-2,5-diones. The introduction chapter describes the mechanisms of action of antiepileptic drugs and the newest anticonvulsant active compounds being currently in different stages of clinical trials. In the experimental section the synthesis of 102 new derivatives of pyrrolidyne-2,5-dione has been described. Major structural modifications are related to the position 1 and 3 of the pyrrolidine-2,5-dione. The primary objective of this study was to examine the impact of the new structural modifications of piperazine derivatives of 3,3-disubstituted pyrrolidine-2,5-dione for anticonvulsant activity. The initial anticonvulsant evaluation was performed within the ADD program in Epilepsy Branch, (NIH/NINDS), USA. Most of the obtained compounds inhibited the electrical convulsion. For selected compounds (with ethylene or propylene spacer between imide and piperazine nitrogen atoms) their 5-HT1A and 5-HT7 serotonin affinities were determined. To explain the possible mechanism of action for the most active compounds the influence on NAv1.2 sodium channel currents were evaluated. In addition for chosen derivatives the lipophilicity was determined using the RP-TLC and computer’s programs which enabled assessment of correlation between the lipophilicity and anticonvulsant activity ; .-
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Last modified:
Mar 13, 2023
In our library since:
Apr 22, 2013
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30
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All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/3496
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| Edition name | Date |
|---|---|
| ZB-118384 | Mar 13, 2023 |
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