Discovery of novel 1,2,3-triazole oseltamivir derivatives as potent influenza neuraminidase inhibitors targeting the 430-cavity

Clicks: 338
ID: 80161
2020
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Overall Quality Improving Quality
71.1 /100
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AI Quality Assessment 🥈 High Quality
83.0 /100
Academic Rigor 88.0%
Novelty 78.0%
Clarity 87.0%
Key Strengths
  • Identification of novel compounds with anti-influenza activity
  • Comprehensive evaluation of compounds against multiple influenza strains
  • Detailed structure-activity relationship (SAR) analysis
Areas for Improvement
  • Limited in vivo data (only embryonated egg model)
  • Comparison to oseltamivir carboxylate could be more extensive
  • Mechanism of action beyond neuraminidase inhibition not fully explored
AI Recommendations

Future studies could focus on in vivo efficacy and safety in mammalian models. Further investigation into the mechanism of action beyond neuraminidase inhibition could also strengthen the findings. A more detailed comparison of the novel compounds with oseltamivir carboxylate in terms of pharmacokinetic properties would be beneficial.

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Real-world Applications
75%
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Ranked #89 of 406 articles by views in European journal of medicinal chemistry

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Abstract
A novel series of 1,2,3-triazole oseltamivir derivatives, which could simultaneously occupy the classical NA catalytic site and the newly reported 430-cavity, were designed, synthesized, and evaluated for their anti-influenza activities. The results demonstrated that four compounds (6g, 6l, 6y and 8c) showed robust anti-influenza potencies against H5N1, H5N2 and H5N6 strains in both enzymatic assay and cellular assay. Especially, 6l was proved to possess the most potent and broad-spectrum anti-influenza activity, with IC50 values of 0.12 μM, 0.049 μM and 0.16 μM and EC50 values of 2.45 μM, 0.43 μM and 2.8 μM against H5N1, H5N2 and H5N6 strains, respectively, which were slightly weaker than oseltamivir carboxylate. In addition, in the embryonated egg model, 6l achieved the similar protective effect against H9N2 strain with oseltamivir carboxylate in the tested concentrations. Preliminary structure-activity relationships (SARs), molecular modeling, and calculated physicochemical properties of selected compounds were also discussed.
Reference Key
ju2020discoveryeuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Han Ju; Siyu Xiu; Xiao Ding; Min Shang; RuiFang Jia; Bing Huang; Peng Zhan; Xinyong Liu
Journal European journal of medicinal chemistry
Year 2020
DOI
10.1016/j.ejmech.2019.111940
URL
https://www.sciencedirect.com/science/article/abs/pii/S022352341931092X?via%3Dihub
Keywords
triazole derivatives influenza neuraminidase inhibitors oseltamivir antiviral activity drug design

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