期刊
CHEMICO-BIOLOGICAL INTERACTIONS
卷 307, 期 -, 页码 16-20出版社
ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2019.04.020
关键词
Organophosphorus compounds; Quaternary oxime; Reactivators; Cholinesterase; Pseudo-catalytic scavenger
资金
- Croatian Science Foundation [IP-2018-01-7683]
- Czech Science Foundation [18-01734S]
Bispyridinium oximes with one (K865, K866, K867) or two (K868, K869, K870) ortho-positioned chlorine moiety, analogous to previously known K027, K048 and K203 oximes, and potent reactivators of human acetylcholinesterase (AChE) inhibited by nerve agents, were tested in the reactivation of human butyrylcholinesterase (BChE) inhibited by sarin, cyclosarin, VX, and tabun. A previously highlighted AChE reactivator, dichlorinated bispyridinium oxime with propyl linker (K868), was tested in more detail for reactivation of four nerve agent-BChE conjugates. Its BChE reactivation potency was showed to be promising when compared to the standard oximes used in medical practice, asoxime (HI-6) and pralidoxime (2-PAM), especially in case of sarin and tabun. This finding could be used in the pseudo-catalytic scavenging of the most nerve agents due to its cumulative capacity to reactivate both AChE and BChE.
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