Synteza a in vitro testovani inhibitoru acetylcholinesterasy bis-4-fenylpyridinioveho typu.

• Main Author: Pilchová, Olga
• Other Authors: Doležal, Martin
• Format: Dissertation
• Language: Czech
• Published: 2012
• Online Access: http://www.nusl.cz/ntk/nusl-308286

Synthesis and in vitro screening of bis-4-phenylpyridinium acetylcholinesterase inhibitors ABSTRACT Organophosphorous compounds are nowadays worldwide used as pesticides and may be misused as highly potent chemical warfare agents. Reversible carbamate inhibitors are used as a pre-exposure treatment for prevention of organophosphorous poisoning. Carbamates bind reversibly to cholinesterase active site and protect it against irreversible damage by OP inhibition. However, carbamates cause numerous adverse effects and are not enough selective. The aim of this thesis was to prepare compounds, which would have potentially better biological properties. During this thesis, twenty potential inhibitors of AChE were prepared and their inhibitory activity towards AChE and BChE was tested in vitro. Subsequently, their activity was compared to standards (cholinesterase selective inhibitors BW284c51 and ethopropazine). Each of prepared compounds showed certain inhibitory activity against both esterases, none of them exceeded efficacy BW284c51 for AChE inhibition. Ten compounds were more effective in BChE inhibition compared to ethopropazine, but they displayed not enough selectivity.