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Synthesis of SARS-CoV-2 M<sup>pro</sup> inhibitors bearing a cinnamic ester warhead with <i>in vitro</i> activity against human coronaviruses

Andrea Citarella, Davide Moi, Martina Pedrini, Helena Pérez‐Peña, Stefano Pieraccini, Alessandro Dimasi, Claudio Stagno, Nicola Micale, Tanja Schirmeister, Giulia Sibille, Giorgio Gribaudo, Alessandra Silvani, Clelia Giannini, Daniele Passarella

2023Organic & Biomolecular Chemistry26 citationsDOIOpen Access PDF

Abstract

A panel of novel cinnamic ester derivatives showed a potent inhibitory effect against SARS-CoV-2 M pro and efficiently impaired the in vitro replication of two human coronaviruses in the low micromolar range.

Topics & Concepts

ChemistryIn vitroSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)CoronavirusCoronavirus disease 2019 (COVID-19)VirologyCinnamic acidViral replication2019-20 coronavirus outbreakStereochemistryBiochemistryVirusBiologyPathologyOutbreakMedicineInfectious disease (medical specialty)DiseaseComputational Drug Discovery MethodsSARS-CoV-2 and COVID-19 ResearchSynthesis and biological activity
Synthesis of SARS-CoV-2 M<sup>pro</sup> inhibitors bearing a cinnamic ester warhead with <i>in vitro</i> activity against human coronaviruses | Litcius