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

Authors :
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
Source :
Scientific Reports, Vol 14, Iss 1, Pp 1-16 (2024)
Publication Year :
2024
Publisher :
Nature Portfolio, 2024.

Abstract

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

Subjects

Subjects :
Medicine
Science

Details

Language :
English
ISSN :
20452322
Volume :
14
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Scientific Reports
Publication Type :
Academic Journal
Accession number :
edsdoj.01b592981ca41dcbf917ad582e8025a
Document Type :
article
Full Text :
https://doi.org/10.1038/s41598-024-59442-4