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
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 Kralove: University of Defence, Faculty of Military Health Sciences, Czech Republic, 2018. str. 38-38 (pozvano predavanje, međunarodna recenzija, sažetak, znanstveni)
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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 Kralove : University of Defence, Faculty of Military Health Sciences, Czech Republic, 2018, 38-38
Skup
13th International Meeting on Cholinesterases ; 7th International Conference on Paraoxonases
Mjesto i datum
Hradec Králové, Češka Republika, 09.09.2018. - 14.09.2018
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
Projekti:
HRZZ-IP-2013-11-4307 - Dizajn, sinteza i evaluacija novih protuotrova kod trovanja živčanim bojnim otrovima i pesticidima (CHOLINESTERASE) (Kovarik, Zrinka, HRZZ - 2013-11) ( CroRIS)
Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb
