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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...
Autores principales: | , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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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. |
format | Online Article Text |
id | pubmed-6843506 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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