Statine-based peptidomimetic compounds as inhibitors for SARS-CoV-2 main protease (SARS-CoV‑2 Mpro)

Autor: Pedro Henrique R. de A. Azevedo, Priscila G. Camargo, Larissa E. C. Constant, Stephany da S. Costa, Celimar Sinézia Silva, Alice S. Rosa, Daniel D. C. Souza, Amanda R. Tucci, Vivian N. S. Ferreira, Thamara Kelcya F. Oliveira, Nathalia R. R. Borba, Carlos R. Rodrigues, Magaly G. Albuquerque, Luiza R. S. Dias, Rafael Garrett, Milene D. Miranda, Diego Allonso, Camilo Henrique da S. Lima, Estela Maris F. Muri
Jazyk: angličtina
Rok vydání: 2024
Předmět:
Zdroj: Scientific Reports, Vol 14, Iss 1, Pp 1-16 (2024)
Druh dokumentu: article
ISSN: 2045-2322
DOI: 10.1038/s41598-024-59442-4
Popis: Abstract COVID-19 is a multisystemic disease caused by the SARS-CoV-2 airborne virus, a member of the Coronaviridae family. It has a positive sense single-stranded RNA genome and encodes two non-structural proteins through viral cysteine-proteases processing. Blocking this step is crucial to control virus replication. In this work, we reported the synthesis of 23 statine-based peptidomimetics to determine their ability to inhibit the main protease (Mpro) activity of SARS-CoV-2. Among the 23 peptidomimetics, 15 compounds effectively inhibited Mpro activity by 50% or more, while three compounds (7d, 8e, and 9g) exhibited maximum inhibition above 70% and IC50
Databáze: Directory of Open Access Journals
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