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SYNTHESIS OF INDOLE-BASED FERULIC ACID DERIVATIVES AND IN VITRO EVALUATION OF ANTIVIRAL ACTIVITY AGAINST SARS-COV-2.
Coronavirus disease
Ferulic acid derivatives
Indole derivatives
SARS-CoV-2
Autor
Verzola, Marina Marina Mol Sena Andrade
Marques, Daisymara Priscila de Almeida
Silva, Elany Barbosa da
Serafim, Mateus Sá Magalhães
Ferreira, Rafaela Salgado
Fajtová, Pavla
Kohlhoff, Markus
O’Donoghue, Anthony John
Maltarollo, Vinícius Gonçalves
Reis, Jordana Grazziela Alves Coelho dos
Oliveira, Renata Barbosa de
Marques, Daisymara Priscila de Almeida
Silva, Elany Barbosa da
Serafim, Mateus Sá Magalhães
Ferreira, Rafaela Salgado
Fajtová, Pavla
Kohlhoff, Markus
O’Donoghue, Anthony John
Maltarollo, Vinícius Gonçalves
Reis, Jordana Grazziela Alves Coelho dos
Oliveira, Renata Barbosa de
Afiliación
Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil/Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Department of Biochemistry and Immunology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Chemistry of Natural Bioactive Products. René Rachou Institute. Oswaldo Cruz Foundation. Belo Horizonte, MG, Brazil
Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil/Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Department of Biochemistry and Immunology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Chemistry of Natural Bioactive Products. René Rachou Institute. Oswaldo Cruz Foundation. Belo Horizonte, MG, Brazil
Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA
Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil
Resumen en ingles
The search for an effective small molecule against the severe acute respiratory syndrome related coronavirus 2 (SARS-CoV2) is a challenge that remains even after the end of the Coronavirus disease 2019 (COVID-19) global health emergency. The indole-based ferulic acid derivatives were synthesized in this work and evaluated for their in vitro cytotoxic profiles and antiSARS-CoV-2 activity. Compounds 1 and 2 decreased the number of genomic copies of SARS-CoV-2 in a dose-dependent manner, with IC50 values of 70.85 µM and 68.28 µM, respectively, with no significant cytotoxicity up to 100 µM against uninfected Vero cells. In order to search for a possible molecular target of these compounds, their activity against the two SARS-CoV-2 cysteine proteases, Mpro and PLpro, in addition to the human cysteine protease cathepsin L (hCatL) was investigated. However, they did not display significant activity against any of these proteases and, therefore, their mechanism of action remains unclear. Our findings suggest that the activity may be related to antioxidant properties of 1 and 2, since the presence of a phenolic group is critical for the antiviral activity.
Palabras clave en ingles
Antiviral activityCoronavirus disease
Ferulic acid derivatives
Indole derivatives
SARS-CoV-2
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