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Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors.
Stille, Julia K; Tjutrins, Jevgenijs; Wang, Guanyu; Venegas, Felipe A; Hennecker, Christopher; Rueda, Andrés M; Sharon, Itai; Blaine, Nicole; Miron, Caitlin E; Pinus, Sharon; Labarre, Anne; Plescia, Jessica; Burai Patrascu, Mihai; Zhang, Xiaocong; Wahba, Alexander S; Vlaho, Danielle; Huot, Mitchell J; Schmeing, T Martin; Mittermaier, Anthony K; Moitessier, Nicolas.
  • Stille JK; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Tjutrins J; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Wang G; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Venegas FA; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Hennecker C; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Rueda AM; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Sharon I; Department of Biochemistry, McGill University, 3649 Promenade Sir William Osler Montreal, QC, Canada, H3G 0B1.
  • Blaine N; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Miron CE; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Pinus S; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Labarre A; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Plescia J; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Burai Patrascu M; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Zhang X; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Wahba AS; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Vlaho D; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Huot MJ; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8.
  • Schmeing TM; Department of Biochemistry, McGill University, 3649 Promenade Sir William Osler Montreal, QC, Canada, H3G 0B1.
  • Mittermaier AK; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8. Electronic address: anthony.mittermaier@mcgill.ca.
  • Moitessier N; Department of Chemistry, McGill University, 801 Sherbrooke St W, Montreal, QC, Canada, H3A 0B8. Electronic address: nicolas.moitessier@mcgill.ca.
Eur J Med Chem ; 229: 114046, 2022 Feb 05.
Article in English | MEDLINE | ID: covidwho-1768050
ABSTRACT
Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Protease Inhibitors / Coronavirus 3C Proteases / COVID-19 Drug Treatment Type of study: Experimental Studies Limits: Animals / Humans Language: English Journal: Eur J Med Chem Year: 2022 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Protease Inhibitors / Coronavirus 3C Proteases / COVID-19 Drug Treatment Type of study: Experimental Studies Limits: Animals / Humans Language: English Journal: Eur J Med Chem Year: 2022 Document Type: Article