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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

Malinak, Davis ; Zorbaz, Tamara ; Skarka, Adam ; Hrabinova, Martina ; Marakovic, Nikola ; Janockova, Jana ; Soukup, Ondrej ; Misik, Jan ; Jun, Daniel ; Kuca, Kamil et al. Oximes with ortho-positioned chlorine moiety exhibit improved physical-chemical properties, efficient reactivation of inhibited human acetylcholinesterase and reduced in vivo toxicity // Vojenské zdravotnické listy / Korábečný, Jan ; Soukup, Ondrej (ur.). 2018. str. 38-38

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

Povezanost rada

Kemija, Javno zdravstvo i zdravstvena zaštita, Farmacija

Poveznice