Novel Inhibitors for COVID

About

Novel Main Protease Inhibitors as SARS-CoV-2 Antivirals Tech ID: UA21-195 Invention: This technology encompasses the development of novel inhibitors for the main protease, or Mpro, of SARS-CoV-2. The main protease of SARS-CoV-2 is a validated drug target and could be key to the development of antiviral drugs against the virus. The inhibitors proposed in this technology are notable, as they are potent main protease inhibitors with high enzymatic inhibition and antiviral activity against SARS-CoV-2. Background: The COVID-19 pandemic caused by the SARS-CoV-2 virus has brought forth an urgent need for novel drugs and therapeutics to help fight the novel disease. Demand for an effective and safe antiviral drug has been extremely high throughout the pandemic. One possible drug target that various researchers have identified is the main protease- or “Mpro” of the SARS-CoV-2. The main protease is key to the viral life cycle, as it allows for the virus to make functional viral proteins and replicate. The majority of current antiviral drugs target the SARS-CoV-2 main protease by modification of a cysteine residue by reactive warhead. This technology proposes and tests small molecule inhibitors based on the superimposed X-ray crystal structures of SARS-CoV-2 Mpro with GC-376, telaprevir, and boceprevir that inhibit the same protease. When compared to existing inhibitors such as GC-376, these had more potent antiviral activity and higher selectivity indexes.