Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Más filtros











Base de datos
Intervalo de año de publicación
1.
Arch Toxicol ; 98(10): 3397-3407, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39004640

RESUMEN

The risk of the use of toxic chemicals for unlawful acts has been a matter of concern for different governments and multilateral agencies. The Organisation for the Prohibition of Chemical Weapons (OPCW), which oversees the implementation of the Chemical Weapons Convention (CWC), considering recent events employing chemical warfare agents as means of assassination, has recently included in the CWC "Annex on Chemicals" some organophosphorus compounds that are regarded as acting in a similar fashion to the classical G- and V-series of nerve agents, inhibiting the pivotal enzyme acetylcholinesterase. Therefore, knowledge of the activity of the pyridinium oximes, the sole class of clinically available acetylcholinesterase reactivators to date, is plainly justified. In this paper, continuing our research efforts in medicinal chemistry on this class of toxic chemicals, we synthesized an A-230 nerve agent surrogate and applied a modified Ellman's assay to evaluate its ability to inhibit our enzymatic model, acetylcholinesterase from Electrophorus eel, and if the clinically available antidotes are able to rescue the enzyme activity for the purpose of relating the findings to the previously disclosed in silico data for the authentic nerve agent and other studies with similar A-series surrogates. Our experimental data indicates that pralidoxime is the most efficient compound for reactivating acetylcholinesterase inhibited by A-230 surrogate, which is the opposite of the in silico data previously disclosed.


Asunto(s)
Acetilcolinesterasa , Sustancias para la Guerra Química , Inhibidores de la Colinesterasa , Reactivadores de la Colinesterasa , Agentes Nerviosos , Oximas , Compuestos de Piridinio , Oximas/farmacología , Acetilcolinesterasa/metabolismo , Reactivadores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/toxicidad , Compuestos de Piridinio/farmacología , Sustancias para la Guerra Química/toxicidad , Agentes Nerviosos/toxicidad , Compuestos de Pralidoxima/farmacología , Compuestos Organotiofosforados/toxicidad , Animales , Antídotos/farmacología
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA