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Pregled bibliografske jedinice broj: 957561

Oximes with ortho-positioned chlorine moiety exhibit improved physical-chemical properties, efficient reactivation of inhibited human acetylcholinesterase and reduced in vivo toxicity


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 // Programme and Abstract Book, Military Medical Science Letters - Special Issue on the occasion of the 13th International Meeting on Cholinesterases and the 7th International Conference on Paraoxonases, Hradec Králové, Republika Češka, 2018 / Korábečný, Jan ; Soukup, Ondrej (ur.).
Hradec Králové, Republika Češka: University of Defence, Faculty of Military Health Sciences, Czech Republic, 2018. str. 38-38 (pozvano predavanje, međunarodna recenzija, sažetak, znanstveni)


Naslov
Oximes with ortho-positioned chlorine moiety exhibit improved physical-chemical properties, efficient reactivation of inhibited human acetylcholinesterase and reduced in vivo toxicity

Autori
Malinak, Davis ; Zorbaz, Tamara ; Skarka, Adam ; Hrabinova, Martina ; Marakovic, Nikola ; Janockova, Jana ; Soukup, Ondrej ; Misik, Jan ; Jun, Daniel ; Kuca, Kamil ; Kovarik, Zrinka ; Musilek, Kamil

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Programme and Abstract Book, Military Medical Science Letters - Special Issue on the occasion of the 13th International Meeting on Cholinesterases and the 7th International Conference on Paraoxonases, Hradec Králové, Republika Češka, 2018 / Korábečný, Jan ; Soukup, Ondrej - Hradec Králové, Republika Češka : University of Defence, Faculty of Military Health Sciences, Czech Republic, 2018, 38-38

Skup
The 13th International Meeting on Cholinesterases and the 7th International Conference on Paraoxonases

Mjesto i datum
Hradec Králové, Češka Republika ; University of Defence, Faculty of Military Health Sciences, Czech Republic, 9.-14.9.2018

Vrsta sudjelovanja
Pozvano predavanje

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
Organophosphate poisoning, chlorinated oximes

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Javno zdravstvo i zdravstvena zaštita, Farmacija



POVEZANOST RADA


Projekt / tema
HRZZ-IP-2013-11-4307 - Dizajn, sinteza i evaluacija novih protuotrova kod trovanja živčanim bojnim otrovima i pesticidima (Zrinka Kovarik, )

Ustanove
Institut za medicinska istraživanja i medicinu rada, Zagreb