Syntéza biskvarterních nesymetrických reaktivátorů acetylcholinesterasy
Stanislav Sopr: PREPARATION OF BISQUARTERNARY NON-SYMETRIC ACETYLCHOLINESTERASE REACTIVATORS Abstract The acetylcholinesterase (AChE) reactivators cause the re-activation of AChE activity after inhibition by organophosphorus compounds (OP). Such OP inhibitors were formerly developed as pesticides, b...
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| Format: | Dissertation |
| Language: | Czech |
| Published: |
2010
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| Online Access: | http://www.nusl.cz/ntk/nusl-280799 |
| Summary: | Stanislav Sopr: PREPARATION OF BISQUARTERNARY NON-SYMETRIC ACETYLCHOLINESTERASE REACTIVATORS Abstract The acetylcholinesterase (AChE) reactivators cause the re-activation of AChE activity after inhibition by organophosphorus compounds (OP). Such OP inhibitors were formerly developed as pesticides, but they were further used as chemical warfare agents due to their extremely high inhibition of cholinesterases. In this diploma thesis, 18 novel AChE reactivators were prepared. Their ability to reactivate paraoxon-inhibited AChE was evaluated in vitro via Ellman's method and compared to 3 standard commercial compounds (pralidoxime, obidoxime and HI-6). Any newly prepared compound was superior to known standards at 10-4 mol/l concentration. However, three novel compounds were able to exceed reactivation ability of known standards at 10-6 mol/l concentration and one novel compound exceeded reactivation limit for further potential in vivo evaluation. |
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