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Structure-Activity Studies Reveal Scope for Optimisation of Ebselen-Type Inhibition of SARS-CoV-2 Main Protease.
Thun-Hohenstein, Siegfried T D; Suits, Timothy F; Malla, Tika R; Tumber, Anthony; Brewitz, Lennart; Choudhry, Hani; Salah, Eidarus; Schofield, Christopher J.
  • Thun-Hohenstein STD; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
  • Suits TF; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
  • Malla TR; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
  • Tumber A; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
  • Brewitz L; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
  • Choudhry H; Department of Biochemistry, Center for Artificial Intelligence in Precision Medicines, King Abdulaziz University, Jeddah, Saudi Arabia.
  • Salah E; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
  • Schofield CJ; Department of Chemistry, University of Oxford, Chemistry Research Laboratory and the Ineos Oxford Institute for Antimicrobial Research, 12 Mansfield Road, Oxford, OX1 3TA, UK.
ChemMedChem ; 17(4): e202100582, 2022 02 16.
Article in English | MEDLINE | ID: covidwho-1540073
ABSTRACT
The reactive organoselenium compound ebselen is being investigated for treatment of coronavirus disease 2019 (COVID-19) and other diseases. We report structure-activity studies on sulfur analogues of ebselen with the Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro ), employing turnover and protein-observed mass spectrometry-based assays. The results reveal scope for optimisation of ebselen/ebselen derivative- mediated inhibition of Mpro , particularly with respect to improved selectivity.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Protease Inhibitors / Organoselenium Compounds / Isoindoles / Coronavirus 3C Proteases / SARS-CoV-2 Limits: Humans Language: English Journal: ChemMedChem Journal subject: Pharmacology / Chemistry Year: 2022 Document Type: Article Affiliation country: Cmdc.202100582

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Protease Inhibitors / Organoselenium Compounds / Isoindoles / Coronavirus 3C Proteases / SARS-CoV-2 Limits: Humans Language: English Journal: ChemMedChem Journal subject: Pharmacology / Chemistry Year: 2022 Document Type: Article Affiliation country: Cmdc.202100582