Discovery of SARS-CoV-2 main protease inhibitors using a synthesis-directed de novo design model

Chem Commun (Camb). 2021 Jun 15;57(48):5909-5912. doi: 10.1039/d1cc00050k.

Abstract

The SARS-CoV-2 main viral protease (Mpro) is an attractive target for antivirals given its distinctiveness from host proteases, essentiality in the viral life cycle and conservation across coronaviridae. We launched the COVID Moonshot initiative to rapidly develop patent-free antivirals with open science and open data. Here we report the use of machine learning for de novo design, coupled with synthesis route prediction, in our campaign. We discover novel chemical scaffolds active in biochemical and live virus assays, synthesized with model generated routes.

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / pharmacology*
  • Coronavirus 3C Proteases / antagonists & inhibitors*
  • Coronavirus OC43, Human / drug effects
  • Cysteine Proteinase Inhibitors / chemical synthesis
  • Cysteine Proteinase Inhibitors / pharmacology*
  • Drug Design
  • Drug Discovery / methods
  • Machine Learning
  • Microbial Sensitivity Tests
  • SARS-CoV-2 / enzymology*

Substances

  • Antiviral Agents
  • Cysteine Proteinase Inhibitors
  • 3C-like proteinase, SARS-CoV-2
  • Coronavirus 3C Proteases