The current pandemic originated by SARS-CoV-2 causes an unprecedented health crisis. The medical world has found itself helpless in the face of this virus, having to deal with the absence of specific effective treatment.

At the time of writing, preventive vaccines are not yet clinically approved, other antiviral drugs have been shown ineffective, and specific drugs addressing SARS-CoV-2 targets are lacking4.

Among all possible viral targets, the virus spike protein/hACE2 interaction has been validated and the design of compounds able to block this interaction upon binding to spike protein is a promising approach.

However, developing a specific drug at a pandemic speed is a hard task especially in the design of a small molecule.

Indeed, beyond the time required for the identification and validation of a lead compound after a library screening, followed by structure-activity relationship studies and clinical development, small molecule drugs are associated with a high attrition rate partly due to their off-target toxicity observed during pharmacological studies.

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