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Eur J Med Chem ; 229: 114046, 2022 Feb 05.
Artículo en Inglés | MEDLINE | ID: covidwho-1768050

RESUMEN

Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.


Asunto(s)
Antivirales/síntesis química , Antivirales/farmacología , Tratamiento Farmacológico de COVID-19 , Proteasas 3C de Coronavirus/antagonistas & inhibidores , Inhibidores de Proteasas/síntesis química , Inhibidores de Proteasas/farmacología , Animales , Diseño de Fármacos , Ensayos Analíticos de Alto Rendimiento , Humanos , Replicación Viral/efectos de los fármacos
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