Oximes with ortho-positioned chlorine moiety exhibit improved physical-chemical properties, efficient reactivation of inhibited human acetylcholinesterase and reduced in vivo toxicity (CROSBI ID 666279)
Prilog sa skupa u časopisu | sažetak izlaganja sa skupa | međunarodna recenzija
Podaci o odgovornosti
Malinak, Davis ; Zorbaz, Tamara ; Skarka, Adam ; Hrabinova, Martina ; Marakovic, Nikola ; Janockova, Jana ; Soukup, Ondrej ; Misik, Jan ; Jun, Daniel ; Kuca, Kamil ; Kovarik, Zrinka ; Musilek, Kamil
engleski
Oximes with ortho-positioned chlorine moiety exhibit improved physical-chemical properties, efficient reactivation of inhibited human acetylcholinesterase and reduced in vivo toxicity
The series of bisquaternary oximes with ortho- positioned chlorine moiety was designed, prepared and evaluated. The novel compounds exhibited valuable pKa properties [1] with improved in vitro reactivation ability of sarin, cyclosarin, VX, paraoxon- and dichlorvos-inhibited human AChE exceeding the standard monoquaternary or bisquaternary reactivators (pralidoxime, methoxime, trimedoxime, obidoxime and asoxime syn. HI-6). Additionally, some chlorinated compounds presented in vitro reactivation ability of tabun-inhibited human AChE similar to the efficiency of trimedoxime. The in vitro results were further explained by molecular docking study. The in vitro non- cytotoxic properties of novel compounds were determined with miscellaneous results. However, assessment of maximum tolerated dose highlighted that the selected chlorinated reactivator is well tolerated by mice on the level similar to the clinically or experimentally used oxime reactivators [2]. The in vivo reactivation study is in progress.
organophosphate poisoning, chlorinated oximes
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Podaci o prilogu
38-38.
2018.
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objavljeno
Podaci o matičnoj publikaciji
Vojenské zdravotnické listy
Korábečný, Jan ; Soukup, Ondrej
Hradec Kralove: University of Defence, Faculty of Military Health Sciences, Czech Republic
0372-7025
Podaci o skupu
13th International Meeting on Cholinesterases ; 7th International Conference on Paraoxonases
pozvano predavanje
09.09.2018-14.09.2018
Hradec Králové, Češka Republika