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Métodos Terapéuticos y Terapias MTCI
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1.
J Gen Virol ; 102(4)2021 04.
Artículo en Inglés | MEDLINE | ID: mdl-33891534

RESUMEN

A small-scale study with Mosi-guard Natural spray, an insect repellent containing Citriodiol, was performed to determine if it has virucidal activity against SARS-CoV-2. A liquid test examined the activity of the insect repellent and the individual components for virucidal activity. A surface contact test looked at the activity of the insect repellent when impregnated on a latex surface as a synthetic skin for potential topical prophylactic application. Both Mosi-guard Natural spray and Citriodiol, as well as other components of the repellent, had virucidal activity in the liquid contact test. On a latex surface used to simulate treated skin, the titre of SARS-CoV-2 was less over time on the Mosi-guard Natural-treated surface but virus was still recovered.


Asunto(s)
Antivirales/uso terapéutico , Tratamiento Farmacológico de COVID-19 , Repelentes de Insectos/uso terapéutico , SARS-CoV-2/efectos de los fármacos , Humanos , Extractos Vegetales/uso terapéutico
2.
J Med Chem ; 49(1): 246-55, 2006 Jan 12.
Artículo en Inglés | MEDLINE | ID: mdl-16392809

RESUMEN

Enzymes that efficiently hydrolyze highly toxic organophosphorus nerve agents could potentially be used as medical countermeasures. As sufficiently active enzymes are currently unknown, we synthesized twelve fluorogenic analogues of organophosphorus nerve agents with the 3-chloro-7-oxy-4-methylcoumarin leaving group as probes for high-throughput enzyme screening. This set included analogues of the pesticides paraoxon, parathion, and dimefox, and the nerve agents DFP, tabun, sarin, cyclosarin, soman, VX, and Russian-VX. Data from inhibition of acetylcholinesterase, in vivo toxicity tests of a representative analogue (cyclosarin), and kinetic studies with phosphotriesterase (PTE) from Pseudomonas diminuta, and a mammalian serum paraoxonase (PON1), confirmed that the analogues mimic the parent nerve agents effectively. They are suitable tools for high-throughput screens for the directed evolution of efficient nerve agent organophosphatases.


Asunto(s)
Acetilcolinesterasa/efectos de los fármacos , Sustancias para la Guerra Química/química , Inhibidores de la Colinesterasa/química , Colorantes Fluorescentes/química , Compuestos Organofosforados/química , Compuestos Organotiofosforados/toxicidad , Hidrolasas de Triéster Fosfórico/química , Animales , Arildialquilfosfatasa/química , Sustancias para la Guerra Química/toxicidad , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/toxicidad , Cumarinas/química , Evaluación Preclínica de Medicamentos/métodos , Cobayas , Hidrólisis , Cinética , Masculino , Estructura Molecular , Compuestos Organofosforados/síntesis química , Compuestos Organofosforados/toxicidad , Compuestos Organotiofosforados/química , Plaguicidas/química , Relación Estructura-Actividad
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