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Synthesis of a novel series of non-symmetrical bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase

Authors :
Kamil Musilek
Kamil Kuca
Ondrej Holas
Martin Dolezal
Daniel Jun
Vlastimil Dohnal
Source :
Journal of Enzyme Inhibition and Medicinal Chemistry. 22:425-432
Publication Year :
2007
Publisher :
Informa UK Limited, 2007.

Abstract

Nine potential non-symmetrical xylene-bridged AChE reactivators were synthesized using modifications of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and the insecticide paraoxon together with nine symmetrical xylene-bridged compounds, was tested in vitro. Seven compounds were promising against paraoxon-inhibited AChE. Two compounds were found to be more potent against tabun-inhibited AChE than obidoxime at a concentration applicable in vivo.

Details

ISSN :
14756374 and 14756366
Volume :
22
Database :
OpenAIRE
Journal :
Journal of Enzyme Inhibition and Medicinal Chemistry
Accession number :
edsair.doi.dedup.....e0c8754578a98138bfbc87b6e257cb0a