Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases

0342827 - ÚCHP 2011 RIV US eng J - Journal Article
Musilová, L. - Jun, D. - Paleček, J. - Církva, Vladimír - Musílek, K. - Paar, M. - Hrabinová, M. - Pohanka, M. - Kuca, K.
Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases.
Letters in Drug Design & Discovery. Roč. 7, č. 4 (2010), s. 260-264. ISSN 1570-1808. E-ISSN 1875-628X
Grant - others:GA MO(CZ) OVUOFVZ200902
Program: OV
Institutional research plan: CEZ:AV0Z40720504
Keywords : acetylcholinesterase * butyrylcholinesterase * nerve agent
Subject RIV: CC - Organic Chemistry
Impact factor: 0.668, year: 2010

New cholinesterase reactivators are synthesized as potential antidotes for treatment of organophosphorus agent poisonings or as part of pseudo catalytic scavengers for improvement of the nerve agent prophylaxis. In this study, three novel potential cholinesterase reactivators (K064 - (E)-1-(pyridinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K065 - (E)-1-(quinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K066 - (E)-1-(isoquinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide) were synthesized and tested for their potency to reactivate acetylcholinesterase (AChE, EC 3.1.1.3) and butyrylcholinesterase (BChE, 3.1.1.8) inhibited by pesticide paraoxon. As resulted, none from the synthesized compounds surpassed currently clinically used reactivators (pralidoxime, obidoxime and HI-6).
Permanent Link: http://hdl.handle.net/11104/0185451