SAR study to find optimal cholinesterase reactivator against organophosphorous nerve agents and pesticides
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61988987%3A17110%2F16%3AA1801RWQ" target="_blank" >RIV/61988987:17110/16:A1801RWQ - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/16:10330207 RIV/60162694:G44__/16:43875688 RIV/62690094:18470/16:50005166
Result on the web
<a href="http://dx.doi.org/10.1007/s00204-016-1827-3" target="_blank" >http://dx.doi.org/10.1007/s00204-016-1827-3</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1007/s00204-016-1827-3" target="_blank" >10.1007/s00204-016-1827-3</a>
Alternative languages
Result language
angličtina
Original language name
SAR study to find optimal cholinesterase reactivator against organophosphorous nerve agents and pesticides
Original language description
Irreversible inhibition of acetylcholinesterase (AChE) by organophosphates leads to many failures in living organism and ultimately in death. Organophosphorus compounds developed as nerve agents such as tabun, sarin, soman, VX and others belong to the most toxic chemical warfare agents and are one of the biggest threats to the modern civilization. Moreover, misuse of nerve agents together with organophosphorus pesticides (e.g. malathion, paraoxon, chlorpyrifos, etc.) which are annually implicated in millions of intoxications and hundreds of thousand deaths reminds us of insufficient protection against these compounds. Basic treatments for these intoxications are based on immediate administration of atropine and acetylcholinesterase reactivators which are currently represented by mono- or bis-pyridinium aldoximes. However, these antidotes are not sufficient to ensure 100 % treatment efficacy even they are administered immediately after intoxication, and in general, they possess several drawbacks. Herein, we have reviewed new efforts leading to the development of novel reactivators and proposition of new promising strategies to design novel and effective antidotes. Structure-activity relationships and biological activities of recently proposed acetylcholinesterase reactivators are discussed and summarized. Among further modifications of known oximes, the main attention has been paid to dual binding site ligands of AChE as the current mainstream strategy. We have also discussed new chemical entities as potential replacement of oxime functional group.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30108 - Toxicology
Result continuities
Project
<a href="/en/project/GA15-16701S" target="_blank" >GA15-16701S: Concept of non-quaternary reactivators AChE as the antidotes of organophsophorus poisoning - a new hope or a blind way?</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
ARCHIVES OF TOXICOLOGY
ISSN
0340-5761
e-ISSN
1432-0738
Volume of the periodical
90
Issue of the periodical within the volume
12
Country of publishing house
DE - GERMANY
Number of pages
29
Pages from-to
2831-2859
UT code for WoS article
000387697600001
EID of the result in the Scopus database
2-s2.0-84984788964