Synthesis and in vitro evaluation of neutral aryloximes as reactivators of Electrophorus eel acetylcholinesterase inhibited by NEMP, a VX surrogate

التفاصيل البيبلوغرافية
العنوان: Synthesis and in vitro evaluation of neutral aryloximes as reactivators of Electrophorus eel acetylcholinesterase inhibited by NEMP, a VX surrogate
المؤلفون: Joyce S. F. D. de Almeida, Ana Beatriz de A. Correa, Alessandro B. C. Simas, Wellington V Dos Santos, Samir F. de A. Cavalcante, Thiago N. da Silva, Leandro B. Bernardo, Tanos C. C. França, Rafael B. Rodrigues, Kamil Kuca, Daniel A. S. Kitagawa
المصدر: Chemico-Biological Interactions. 309:108682
بيانات النشر: Elsevier BV, 2019.
سنة النشر: 2019
مصطلحات موضوعية: 0301 basic medicine, Cholinesterase Reactivators, Pyrrolidines, Antidotes, Central nervous system, Pharmacology, Toxicology, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Oximes, medicine, Animals, Enzyme Reactivation, Nerve agent, Eels, Chemistry, Organothiophosphorus Compounds, General Medicine, Penetration (firestop), Acetylcholinesterase, In vitro, 030104 developmental biology, medicine.anatomical_structure, 030220 oncology & carcinogenesis, Electrophorus, Cholinesterase Inhibitors, Pyridinium, medicine.drug
الوصف: Casualties caused by nerve agents, potent acetylcholinesterase inhibitors, have attracted attention from media recently. Poisoning with these chemicals may be fatal if not correctly addressed. Therefore, research on novel antidotes is clearly warranted. Pyridinium oximes are the only clinically available compounds, but poor penetration into the blood-brain barrier hampers efficient enzyme reactivation at the central nervous system. In searching for structural factors that may be explored in SAR studies, we synthesized and evaluated neutral aryloximes as reactivators for acetylcholinesterase inhibited by NEMP, a VX surrogate. Although few tested compounds reached comparable reactivation results with clinical standards, they may be considered as leads for further optimization.
تدمد: 0009-2797
DOI: 10.1016/j.cbi.2019.05.048
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d768331c82a5d43b8db467912c1a7d40
https://doi.org/10.1016/j.cbi.2019.05.048
Rights: CLOSED
رقم الانضمام: edsair.doi.dedup.....d768331c82a5d43b8db467912c1a7d40
قاعدة البيانات: OpenAIRE
الوصف
تدمد:00092797
DOI:10.1016/j.cbi.2019.05.048