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

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 agai...

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Autores principales: Kitagawa, Daniel A. S., Cavalcante, Samir F. de A., de Paula, Reuel L., Rodrigues, Rafael B., Bernardo, Leandro B., da Silva, Munique C. J., da Silva, Thiago N., dos Santos, Wellington V., Granjeiro, José M., de Almeida, Joyce S. F. D., Barcellos, Marcos C., de A. Correa, Ana Beatriz, França, Tanos C. C., Kuča, Kamil, Simas, Alessandro B. C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6843506/
https://www.ncbi.nlm.nih.gov/pubmed/31597234
http://dx.doi.org/10.3390/biom9100583
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author Kitagawa, Daniel A. S.
Cavalcante, Samir F. de A.
de Paula, Reuel L.
Rodrigues, Rafael B.
Bernardo, Leandro B.
da Silva, Munique C. J.
da Silva, Thiago N.
dos Santos, Wellington V.
Granjeiro, José M.
de Almeida, Joyce S. F. D.
Barcellos, Marcos C.
de A. Correa, Ana Beatriz
França, Tanos C. C.
Kuča, Kamil
Simas, Alessandro B. C.
author_facet Kitagawa, Daniel A. S.
Cavalcante, Samir F. de A.
de Paula, Reuel L.
Rodrigues, Rafael B.
Bernardo, Leandro B.
da Silva, Munique C. J.
da Silva, Thiago N.
dos Santos, Wellington V.
Granjeiro, José M.
de Almeida, Joyce S. F. D.
Barcellos, Marcos C.
de A. Correa, Ana Beatriz
França, Tanos C. C.
Kuča, Kamil
Simas, Alessandro B. C.
author_sort Kitagawa, Daniel A. S.
collection PubMed
description 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.
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spelling pubmed-68435062019-11-25 In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon Kitagawa, Daniel A. S. Cavalcante, Samir F. de A. de Paula, Reuel L. Rodrigues, Rafael B. Bernardo, Leandro B. da Silva, Munique C. J. da Silva, Thiago N. dos Santos, Wellington V. Granjeiro, José M. de Almeida, Joyce S. F. D. Barcellos, Marcos C. de A. Correa, Ana Beatriz França, Tanos C. C. Kuča, Kamil Simas, Alessandro B. C. Biomolecules Article 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. MDPI 2019-10-08 /pmc/articles/PMC6843506/ /pubmed/31597234 http://dx.doi.org/10.3390/biom9100583 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Kitagawa, Daniel A. S.
Cavalcante, Samir F. de A.
de Paula, Reuel L.
Rodrigues, Rafael B.
Bernardo, Leandro B.
da Silva, Munique C. J.
da Silva, Thiago N.
dos Santos, Wellington V.
Granjeiro, José M.
de Almeida, Joyce S. F. D.
Barcellos, Marcos C.
de A. Correa, Ana Beatriz
França, Tanos C. C.
Kuča, Kamil
Simas, Alessandro B. C.
In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon
title In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon
title_full In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon
title_fullStr In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon
title_full_unstemmed In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon
title_short In Vitro Evaluation of Neutral Aryloximes as Reactivators for Electrophorus eel Acetylcholinesterase Inhibited by Paraoxon
title_sort in vitro evaluation of neutral aryloximes as reactivators for electrophorus eel acetylcholinesterase inhibited by paraoxon
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6843506/
https://www.ncbi.nlm.nih.gov/pubmed/31597234
http://dx.doi.org/10.3390/biom9100583
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