Targeted Synthesis of1-(4-Hydroxyiminomethylpyridinium)-3-pyridiniumpropane Dibromide – A New Nerve Agent Reactivator

Molecules

Kamil Kuca¹  Kamil Musilek²  Martin Paar³  Daniel Jun¹  Petr Stodulka¹  Martina Hrabinova¹ 

[1] Center of Advanced Studies, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic;Department of Toxicology, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic;Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy, Hradec Kralove, Czech Republic

关键词: Acetylcholinesterase;    reactivator;    nerve agent;    broad-spectrum reactivator;   

DOI  :  10.3390/12081964

来源: mdpi

【 摘 要 】

Preparation of 1-(4-hydroxy-iminomethylpyridinium)-3-pyridiniumpropane dibromide is described. This compound represents a new acetylcholinesterase (AChE) reactivator, which has no substituents on the second pyridinium ring as found in other commonly used AChE reactivators. The reactivation ability of this reactivator was tested on tabun- and cyclosarin-inhibited AChE. According to the results obtained, the new compound (without substitution and with decreased molecule size) showed increased reactivation potency in case of cyclosarin inhibited AChE. A potent oxime for treatment of tabun and cyclosarin-caused intoxications was thus obtained via slight modification of the reactivator structure (compared to trimedoxime and K027).

【 授权许可】

Unknown   
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