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In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon

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dc.rights.license CC BY eng
dc.contributor.author Kitagawa, Daniel A. S. cze
dc.contributor.author Cavalcante, Samir cze
dc.contributor.author de Paula, Reuel L. cze
dc.contributor.author Rodrigues, Rafael B. cze
dc.contributor.author Bernardo, Leandro B. cze
dc.contributor.author da Silva, Munique C. J. cze
dc.contributor.author da Silva, Thiago N. cze
dc.contributor.author dos Santos, Wellington, V cze
dc.contributor.author Granjeiro, Jose M. cze
dc.contributor.author de Almeida, Joyce S. F. D. cze
dc.contributor.author Barcellos, Marcos C. cze
dc.contributor.author Correa, Ana Beatriz de A. cze
dc.contributor.author Costa Franca, Tanos Celmar cze
dc.contributor.author Kuča, Kamil cze
dc.contributor.author Simas, Alessandro B. C. cze
dc.date.accessioned 2020-06-07T20:51:03Z
dc.date.available 2020-06-07T20:51:03Z
dc.date.issued 2019 eng
dc.identifier.issn 2218-273X eng
dc.identifier.uri http://hdl.handle.net/20.500.12603/333
dc.description.abstract Casualties caused by organophosphorus pesticides are a burden for health systems in developing and poor countries. Such compounds are potent acetylcholinesterase irreversible inhibitors, and share the toxic profile with nerve agents. Pyridinium oximes are the only clinically available antidotes against poisoning by these substances, but their poor penetration into the blood-brain barrier hampers the efficient enzyme reactivation at the central nervous system. In searching for structural factors that may be explored in future SAR studies, we evaluated neutral aryloximes as reactivators for paraoxon-inhibited Electrophorus eel acetylcholinesterase. Our findings may result into lead compounds, useful for development of more active compounds for emergencies and supportive care. eng
dc.format p. "Article Number: 583" eng
dc.language.iso eng eng
dc.publisher MDPI eng
dc.relation.ispartof BIOMOLECULES, volume 9, issue: 10 eng
dc.subject acetylcholinesterase eng
dc.subject pesticides eng
dc.subject neutral oximes eng
dc.subject antidotes eng
dc.subject drug design eng
dc.subject acetylcholinesteráza cze
dc.subject pesticidy cze
dc.subject neutrální oximy cze
dc.subject antidota cze
dc.subject design léků cze
dc.title In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon eng
dc.title.alternative Hodnocení in vitro neutrálních aryloximů jako reaktivátorů pro úhoře acetylcholinesterázy úhořů elektroforem inhibovaných paraoxonem cze
dc.type article eng
dc.identifier.obd 43875732 eng
dc.identifier.wos 000497726800075 eng
dc.identifier.doi 10.3390/biom9100583 eng
dc.description.abstract-translated Casualties caused by organophosphorus pesticides are a burden for health systems in developing and poor countries. Such compounds are potent acetylcholinesterase irreversible inhibitors, and share the toxic profile with nerve agents. Pyridinium oximes are the only clinically available antidotes against poisoning by these substances, but their poor penetration into the blood-brain barrier hampers the efficient enzyme reactivation at the central nervous system. In searching for structural factors that may be explored in future SAR studies, we evaluated neutral aryloximes as reactivators for paraoxon-inhibited Electrophorus eel acetylcholinesterase. Our findings may result into lead compounds, useful for development of more active compounds for emergencies and supportive care. cze
dc.publicationstatus postprint eng
dc.peerreviewed yes eng
dc.source.url https://www.mdpi.com/2218-273X/9/10/583 cze
dc.relation.publisherversion https://www.mdpi.com/2218-273X/9/10/583 eng
dc.rights.access Open Access eng


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