Novel Bisquaternary Oximes—Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon

Molecules

Kamil Kuca¹  Lucie Musilova¹  Jiri Palecek¹  Vladimir Cirkva¹  Martin Paar¹  Kamil Musilek¹  Martina Hrabinova¹  Miroslav Pohanka¹  Jana Zdarova Karasova¹ 

[1] ¹Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic

关键词: acetylcholinesterase;    butyrylcholinesterase;    reactivator;    nerve agent;    oxime;    pesticide;    scavenger;   

DOI  :  10.3390/molecules14124915

来源: mdpi

【 摘 要 】

Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyrylcholinesterase (BuChE; EC 3.1.1.8) inhibited by paraoxon. Their reactivation activity was compared with standard reactivators—pralidoxime, obidoxime and HI-6—which are clinically used at present. As it resulted, none of the prepared compounds surpassed obidoxime, which is considered to be the most potent compound if used for reactivation of AChE inhibited by paraoxon. In case of BuChE reactivation, two compounds (K053 and K068) achieved similar results as obidoxime.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.