ArticleBioorganic chemistry2021
The Mpro structure-based modifications of ebselen derivatives for improved antiviral activity against SARS-CoV-2 virus.
Article in Bioorganic chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 38 citations in OpenAlex.
- Insights into the complexity of SARS-CoV-2 MJournal of enzyme inhibition and medicinal chemistry · 2026Article
- Broad-spectrum antiviral activity of ebselen.Scientific reports · 2025Article
- Article
- New insights in the mechanism of the SARS-CoV-2 MScientific reports · 2024Article
- Repurposing the Open Global Health Library for the discovery of novel Mpro destabilizers with scope as broad-spectrum antivirals.Frontiers in pharmacology · 2024Article
- Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy.International journal of nanomedicine · 2024Review
- Structure and function of SARS-CoV and SARS-CoV-2 main proteases and their inhibition: A comprehensive review.European journal of medicinal chemistry · 2023Review
- Ebselen and Diphenyl Diselenide Inhibit SARS-CoV-2 Replication at Non-Toxic Concentrations to Human Cell Lines.Vaccines · 2023Article
- Ebselen derivatives inhibit SARS-CoV-2 replication by inhibition of its essential proteins: PLScientific reports · 2023Article
- Optimized Ebselen-Based Inhibitors of Bacterial Ureases with Nontypical Mode of Action.Journal of medicinal chemistry · 2023Article
- Detailed Insights into the Inhibitory Mechanism of New Ebselen Derivatives against Main Protease (MACS pharmacology & translational science · 2023Article
- The SARS-CoV-2 main protease (MMedComm · 2022Review
- Synthesis and crystal structures of new mixed-ligand schiff base complexes containingPolyhedron · 2022Article
- Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease.Journal of medicinal chemistry · 2022Review
- Advances in the Development of SARS-CoV-2 Mpro Inhibitors.Molecules (Basel, Switzerland) · 2022Review
- Electrochemical Biosensor for the Detection of SARS-CoV-2 Main Protease and Its Inhibitor Ebselen.International journal of electrochemical science · 2022Article
- Progress on SARS-CoV-2 3CLpro Inhibitors: Inspiration from SARS-CoV 3CLpro Peptidomimetics and Small-Molecule Anti-Inflammatory Compounds.Drug design, development and therapy · 2022Review
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The main protease (Mpro or 3CLpro) of SARS-CoV-2 virus is a cysteine enzyme critical for viral replication and transcription, thus indicating a potential target for antiviral therapy. A recent repurposing effort has identified ebselen, a multifunctional drug candidate as an inhibitor of Mpro. Our docking of ebselen to the binding pocket of Mpro crystal structure suggests a noncovalent interaction for improvement of potency, antiviral activity and selectivity. To test this hypothesis, we designed and synthesized ebselen derivatives aimed at enhancing their non-covalent bonds within Mpro. The inhibition of Mpro by ebselen derivatives (0.3 μM) was screened in both HPLC and FRET assays. Nine ebselen derivatives (EBs) exhibited stronger inhibitory effect on Mpro with IC
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.