Molecules (Apr 2022)

Advances in the Development of SARS-CoV-2 Mpro Inhibitors

  • Laura Agost-Beltrán,
  • Sergio de la Hoz-Rodríguez,
  • Lledó Bou-Iserte,
  • Santiago Rodríguez,
  • Adrián Fernández-de-la-Pradilla,
  • Florenci V. González

DOI
https://doi.org/10.3390/molecules27082523
Journal volume & issue
Vol. 27, no. 8
p. 2523

Abstract

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Since the outbreak of COVID-19, one of the strategies used to search for new drugs has been to find inhibitors of the main protease (Mpro) of the virus SARS-CoV-2. Initially, previously reported inhibitors of related proteases such as the main proteases of SARS-CoV and MERS-CoV were tested. A huge effort was then carried out by the scientific community to design, synthesize and test new small molecules acting as inactivators of SARS-CoV-2 Mpro. From the chemical structure view, these compounds can be classified into two main groups: one corresponds to modified peptides displaying an adequate sequence for high affinity and a reactive warhead; and the second is a diverse group including chemical compounds that do not have a peptide framework. Although a drug including a SARS-CoV-2 main protease inhibitor has already been commercialized, denoting the importance of this field, more compounds have been demonstrated to be promising potent inhibitors as potential antiviral drugs.

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