ArticleBioorganic chemistry2021
Discovery of novel oxazole-based macrocycles as anti-coronaviral agents targeting SARS-CoV-2 main protease.
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 11 papers.
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Who cites it
11 citing papers in PubMed, 21 citations in OpenAlex.
- Design, synthesis, and antibacterial efficacy of new methylene disalicylic acid/1,3,4-oxadiazole hybrids as dual inhibitors of DNA gyrase and topoisomerase IV.Molecular diversity · 2026Article
- Structure-activity relationship and molecular docking analysis of novel arylhydrazones of imidazodiazabicycloalkanones with antibacterial properties.Molecular diversity · 2026Article
- Exploring Macrocyclic Chemical Space: Strategies and Technologies for Drug Discovery.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Recent Advancements in the Synthetic Chemistry of Oxazole Derivatives and their Significant Medicinal Applications.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Identification of a macrocyclic compound targeting the lassa virus polymerase.Antiviral research · 2024Article
- Discovery of new Schiff bases of the disalicylic acid scaffold as DNA gyrase and topoisomerase IV inhibitors endowed with antibacterial properties.Frontiers in chemistry · 2024Article
- Synthesis, enzyme inhibition, and docking studies of new schiff bases of disalicylic acid methylene-based derivatives as dual-target antibacterial agents.Frontiers in chemistry · 2024Article
- Small molecules in the treatment of COVID-19.Signal transduction and targeted therapy · 2022Review
- The SARS-CoV-2 main protease (MMedComm · 2022Review
- Microbial Natural Products with Antiviral Activities, Including Anti-SARS-CoV-2: A Review.Molecules (Basel, Switzerland) · 2022Review
- Hydroxamate and thiosemicarbazone: Two highly promising scaffolds for the development of SARS-CoV-2 antivirals.Bioorganic chemistry · 2022Article
Corrections and comments
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Authors and funding
16 authors at 8 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have discovered a family of synthetic oxazole-based macrocycles to be active against SARS-CoV-2. The synthesis, pharmacological properties, and docking studies of the compounds are reported in this study. The structure of the new macrocycles was confirmed by NMR spectroscopy and mass spectrometry. Compounds 13, 14, and 15a-c were evaluated for their anti-SARS-CoV-2 activity on SARS-COV-2 (NRC-03-nhCoV) virus in Vero-E6 cells. Isopropyl triester 13 and triacid 14 demonstrated superior inhibitory activities against SARS-CoV-2 compared to carboxamides 15a-c. MTT cytotoxicity assays showed that the CC
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Registered trials
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