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Tytuł: Structure - anticonvulsant activity relationship in the group of aminoalkanol derivatives
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The main aim of the performed research was determination of structure - anticonvulsant activity relationship in the group of selected aminoalkanol derivatives.In the introduction to the thesis there were discussed general issues concerning currently used antiepileptic drugs as well as progress in discovering new substances with anticonvulsant activity.The performed research constituted synthesis of 59 compounds which were derivatives of N-(trans)-cinnamyl or N-(trans)-cinnamoyl derivatives of aminoalkanol as well as selected derivatives obtained by means of chemical or biotechnological modifications. The thesis includes the detailed description of the synthesis of the compounds, physicochemical analyzes (e.g. spectral, lipophylicity and pKa determination) as well as in silico evaluation (metabolism prediction, calculation ofZał. nr 1 do § 2 zarządzenia nr 45Rektora UJ z 12 czerwca 2006 rokustructural descriptors).All synthesized compounds were submitted to the anticonvulsant activity evaluation (carried out at NIH, USA). 54 substances proved their activity in at least one of the animal seizure models. Based on the performed pharmacological tests a structure - anticonvulsant activity relationship in the investigated group of compounds was established. The aminoalkanol moiety may be relevant for anaticonvulsant activity (2-aminopropan-1-ol, 1-aminopropan-2-ol, 1-aminobutan-2-ol, ; 3-hydroxypiperidine were favorable aminoalkanols). In case of alkanoloamide derivatives of (trans)-cinnamic acid the preferable position of methyl residue in phenyl ring was orto when compared to para.
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Data ostatniej modyfikacji:
14 mar 2023
Data dodania obiektu:
7 kwi 2015
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http://dl.cm-uj.krakow.pl:8080/publication/3979
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| Nazwa wydania | Data |
|---|---|
| ZB-119630 | 14 mar 2023 |
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