Determination of reactivation potency for DFP- and paraoxon-inhibited acetylcholinesterases by pyridinium oximes

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F08%3A00001946" target="_blank" >RIV/60162694:G44__/08:00001946 - isvavai.cz</a>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

Determination of reactivation potency for DFP- and paraoxon-inhibited acetylcholinesterases by pyridinium oximes

Original language description

Exposure to the organophosphorus nerve agents such as sarin, soman, cyclosarin, and VX causes acute intoxication by inhibiting acetylcholinesterase (AChE), where the serine residue of the active site can attack the phosphorous atom of the organophosphorus agents to form a strong P-O bond. The purpose of the present study was to evaluate new oxime antidotes to reactivate the inhibited AChE. We have designed and synthesized several new oximes, and have evaluated the substances that differ from the currently used oximes in linker between the two pyridinium rings. The potency of newly synthesized oximes was compared with two currently used AChE reactivators (2-PAM, HI-6). The reactivation potencies of the bis-pyridinium oximes connected with a (CH2)n linker between the two quaternary nitrogen atoms were evaluated with housefly (HF) AChE inhibited by diisopropyl fluorophosphates (DFP) and by paraoxon. The bis-pyridinium oximes showed stronger activity compared with monopyridinium oxime, and

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FP - Other medical fields

OECD FORD branch

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Project

<a href="/en/project/ME%20865" target="_blank" >ME 865: Countermeasure against chemical terrorism - development of new antidotes against nerve agents</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2008

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Chemico-Biological Interactions

ISSN

0009-2797

e-ISSN

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Volume of the periodical

175

Issue of the periodical within the volume

1-3

Country of publishing house

IE - IRELAND

Number of pages

3

Pages from-to

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UT code for WoS article

000260110500070

EID of the result in the Scopus database

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