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Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases
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SYSNO ASEP 0342827 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases Author(s) Musilová, L. (CZ)
Jun, D. (CZ)
Paleček, J. (DE)
Církva, Vladimír (UCHP-M) RID, ORCID, SAI
Musílek, K. (CZ)
Paar, M. (CZ)
Hrabinová, M. (CZ)
Pohanka, M. (CZ)
Kuca, K. (CZ)Source Title Letters in Drug Design & Discovery - ISSN 1570-1808
Roč. 7, č. 4 (2010), s. 260-264Number of pages 5 s. Language eng - English Country US - United States Keywords acetylcholinesterase ; butyrylcholinesterase ; nerve agent Subject RIV CC - Organic Chemistry CEZ AV0Z40720504 - UCHP-M (2005-2011) UT WOS 000275929300006 DOI 10.2174/157018010790945823 Annotation 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). Workplace Institute of Chemical Process Fundamentals Contact Eva Jirsová, jirsova@icpf.cas.cz, Tel.: 220 390 227 Year of Publishing 2011
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