ArticleBioorganic chemistry2021
Discovery and evolution of 12N-substituted aloperine derivatives as anti-SARS-CoV-2 agents through targeting late entry stage.
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 4 papers.
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Who cites it
4 citing papers in PubMed.
- Design, Synthesis and Biological Exploration of NovelInternational journal of molecular sciences · 2024Article
- Aloperine Inhibits ASFV via Regulating PRLR/JAK2 Signaling Pathway In Vitro.International journal of molecular sciences · 2024Article
- Quinolizidines as Novel SARS-CoV-2 Entry Inhibitors.International journal of molecular sciences · 2022Article
- Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism.European journal of medicinal chemistry · 2022Article
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Authors and funding
12 authors.
Funding
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Abstract
So far, there is still no specific drug against COVID-19. Taking compound 1 with anti-EBOV activity as the lead, fifty-four 12N-substituted aloperine derivatives were synthesized and evaluated for the anti-SARS-CoV-2 activities using pseudotyped virus model. Among them, 8a exhibited the most potential effects against both pseudotyped and authentic SARS-CoV-2, as well as SARS-CoV and MERS-CoV, indicating a broad-spectrum anti-coronavirus profile. The mechanism study disclosed that 8a might block a late stage of viral entry, mainly via inhibiting host cathepsin B activity rather than directly targeting cathepsin B protein. Also, 8a could significantly reduce the release of multiple inflammatory cytokines in a time- and dose-dependent manner, such as IL-6, IL-1β, IL-8 and MCP-1, the major contributors to cytokine storm. Therefore, 8a is a promising agent with the advantages of broad-spectrum anti-coronavirus and anti-cytokine effects, thus worthy of further investigation.
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