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Title: Structure - anticonvulsant activity relationship in the group of aminoalkanol derivatives

Abstract:

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.

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmacja ; neurologia

Degree grantor:

Uniwersytet Jagielloński. Collegium Medicum. Wydział Farmaceutyczny. Katedra Chemii Organicznej. Zakład Chemii Bioorganicznej.

Promoter:

Henryk Marona

Date issued:

2012

Format:

application/pdf

Identifier:

oai:dl.cm-uj.krakow.pl:3979

Call number:

ZB-119630

ControlNumberVIRTUA:

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Language:

pol

Access rights:

tylko w bibliotece

Location of original object:

Biblioteka Medyczna Uniwersytetu Jagiellońskiego- Collegium Medicum

Object collections:

Last modified:

Jun 26, 2019

In our library since:

Apr 7, 2015

Number of object content hits:

8

Number of object content views in PDF format

8

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/3979

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ZB-119630 Jun 26, 2019
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