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Monooxime-monocarbamoyl bispyridinium xylene-linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies

Publication at Central Library of Charles University |
2010

Abstract

26 monooxime-monocarbamoyl xylene linked bispyridinium compounds were prepared and tested in vitro along with known reactivators on a model of tabun- and paraoxon-, methylparaoxon- and DFP-inhibited human erythrocyte AChE. Some newly prepared compounds showed promising reactivation of pesticide-inhibited AChE.

The acute toxicity was also determined. Docking studies using tabun-inhibited AChe were performed for 3 compounds.

SAR study confirmed the apparent influence of the xylene-linkage and carbamoyl moiety on the reactivation ability and toxicity of the agents.