78282-91-4Relevant articles and documents
Monooxime bispyridinium reactivators bearing xylene linker synthesis and in vitro evaluation on model of organophosphate-inhibited acetylcholinesterase
Musilek, Kamil,Hambalek, Jan,Holas, Ondrej,Dohnal, Vlastimil,Kuca, Kamil
, p. 362 - 370 (2016/07/06)
Nine novel mono-oxime reactivators bearing xylene linker were synthesized in an effort to improve previously prepared xylene bisoximes and monocarbamoyl-monooximes. The novel compounds were tested in vitro on the model of tabun-, paraoxon-, methylparaoxon
Monooxime-monocarbamoyl bispyridinium xylene-linked reactivators of acetylcholinesterase - synthesis, in vitro and toxicity evaluation, and docking studies
Musilek, Kamil,Holas, Ondrej,Misik, Jan,Pohanka, Miroslav,Novotny, Ladislav,Dohnal, Vlastimil,Opletalova, Veronika,Kuca, Kamil
scheme or table, p. 247 - 254 (2010/12/18)
Acetylcholinesterase (AChE) reactivators are crucial antidotes to organophosphate intoxication. A new series of 26 monooxime-monocarbamoyl xylene-linked bispyridinium compounds was prepared and tested in vitro, along with known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime, K107, K108 and K203), on a model of tabun- and paraoxon-, methylparaoxon- and DFP-inhibited human erythrocyte AChE. Although their ability to reactivate tabun-inhibited AChE did not exceed that of the previously known compounds, some newly prepared compounds showed promising reactivation of pesticide-inhibited AChE. The acute toxicity of the 0ovel compounds was also determined. Docking studies using tabun-inhibited AChE were performed for three compounds of interest. The structure-activity relationship (SAR) study confirmed the apparent influence of the xylene linkage and carbamoyl moiety on the reactivation ability and toxicity of the agents.
