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Title: Synthesis and anticonvulsant activity of some aminoalkanol derivatives
Abstract:
The thesis is part of research in the field of synthesis and anticonvulsant properties of aminoalkanol derivatives realized at the Department of Technology and Biotechnology of Drugs, within the cooperation of The Faculty of Pharmacy with National Institutes of Health (NIH, Bethesda, USA). Due to the cooperation some lead structures had been selected due to their anticonvulsant activity comparable to some known antiepileptic drugs. The aim of the thesis was synthesis of chiral and achiral analogues and/or homologues of the lead structures, assessment of their physical properties and anticonvulsant activity. 52 structures have been synthesized: (4-benzyloxy)benzoil- and [( 4-benzyloxy)benzyl]aminoalkanols (in publication), [(phenoxy)alkyl]- and [(phenoxy)acetyl]aminoalkanols and/ or their aminoacid analogues. Their homogenicity and structure have been verified using elemental analysis, chromatography (TLC) and spectral methods (1R, 1H NMR, 13C NMR, or MS/MS). Pharmacological assays were performed at the NIH. The greatest anticonvulsant activity was observed for some derivatives in the maximal electroshock seizure (MES) test, the Lamotrigine resistant epilepsy model, the audiogenic seizure model and the electric kindling model as well as the pilocarpine-induced status epilepticus. The thesis also contains the following assays, performed for the most active substances: • lipophil ; icity assay (RM0, clog P); • enantiomeric excess assay (%ee); • chemical stability test; • mutagenicity test; • in silico metabolism simulation.
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Last modified:
Feb 16, 2023
In our library since:
Nov 21, 2012
Number of object content hits:
10
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0
All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/1017
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| Edition name | Date |
|---|---|
| ZB-107975 | Feb 16, 2023 |
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