Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice

A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. It was found that aromatic groups coupled to Mannich phenols and the introduction of imidazole to the ortho position of phenols would dramat...

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Autores principales: Wei, Zhao, Zhang, Xinlei, Nie, Huifang, Yao, Lin, Liu, Yanqin, Zheng, Zhibing, Ouyang, Qin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8840479/
https://www.ncbi.nlm.nih.gov/pubmed/35164361
http://dx.doi.org/10.3390/molecules27031096
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author Wei, Zhao
Zhang, Xinlei
Nie, Huifang
Yao, Lin
Liu, Yanqin
Zheng, Zhibing
Ouyang, Qin
author_facet Wei, Zhao
Zhang, Xinlei
Nie, Huifang
Yao, Lin
Liu, Yanqin
Zheng, Zhibing
Ouyang, Qin
author_sort Wei, Zhao
collection PubMed
description A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. It was found that aromatic groups coupled to Mannich phenols and the introduction of imidazole to the ortho position of phenols would dramatically enhance reactivation efficiency. Moreover, the in vivo experiment was conducted, and the results demonstrated that Mannich phenol L10R1 (30 mg/kg, ip) could afford 100% 48 h survival for mice of 2*LD(50) sarin exposure, which is promising for the development of non-oxime reactivators with central efficiency.
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spelling pubmed-88404792022-02-13 Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice Wei, Zhao Zhang, Xinlei Nie, Huifang Yao, Lin Liu, Yanqin Zheng, Zhibing Ouyang, Qin Molecules Article A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. It was found that aromatic groups coupled to Mannich phenols and the introduction of imidazole to the ortho position of phenols would dramatically enhance reactivation efficiency. Moreover, the in vivo experiment was conducted, and the results demonstrated that Mannich phenol L10R1 (30 mg/kg, ip) could afford 100% 48 h survival for mice of 2*LD(50) sarin exposure, which is promising for the development of non-oxime reactivators with central efficiency. MDPI 2022-02-07 /pmc/articles/PMC8840479/ /pubmed/35164361 http://dx.doi.org/10.3390/molecules27031096 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Wei, Zhao
Zhang, Xinlei
Nie, Huifang
Yao, Lin
Liu, Yanqin
Zheng, Zhibing
Ouyang, Qin
Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice
title Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice
title_full Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice
title_fullStr Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice
title_full_unstemmed Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice
title_short Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice
title_sort discovery of novel non-oxime reactivators showing in vivo antidotal efficiency for sarin poisoned mice
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8840479/
https://www.ncbi.nlm.nih.gov/pubmed/35164361
http://dx.doi.org/10.3390/molecules27031096
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