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Related Concept Videos

Influenza01:27

Influenza

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Influenza is an acute, highly communicable viral disease that affects the respiratory tract and is responsible for seasonal epidemics worldwide. Influenza A is the most prevalent type associated with widespread outbreaks and is subtyped based on two surface glycoproteins: hemagglutinin (H) and neuraminidase (N), as in H1N1. These glycoproteins are essential for viral infectivity, transmission, and immune recognition. Transmission occurs primarily through respiratory droplets and contaminated...
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Fluorescence-based Neuraminidase Inhibition Assay to Assess the Susceptibility of Influenza Viruses to The Neuraminidase Inhibitor Class of Antivirals
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Identification of Influenza H1N1 Endonuclease Inhibitor via Virtual Screening and In Vitro Validation.

Shymaa Damfo1

  • 1Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Madinah, Saudi Arabia.

Medicinal Chemistry (Shariqah (United Arab Emirates))
|April 30, 2026
PubMed
Summary

Researchers identified a novel triazole-pyridine derivative as a potent inhibitor of the H1N1 influenza virus polymerase acidic endonuclease. This compound shows promising antiviral activity and a favorable safety profile for developing new influenza therapeutics.

Keywords:
Influenzadrug discoveryendonucleaseinhibitormolecular dockingvirtual screening

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Area of Science:

  • Virology
  • Medicinal Chemistry
  • Computational Chemistry

Background:

  • The H1N1 influenza pandemic poses a significant global health threat, necessitating the development of novel antiviral drugs due to emerging resistant strains.
  • The influenza polymerase acidic (PA) endonuclease is a critical target for antiviral development, essential for viral replication.

Purpose of the Study:

  • To identify novel inhibitors of the H1N1 PA endonuclease using a virtual fragment-based screening approach.
  • To validate the inhibitory activity and cytotoxicity of identified compounds against H1N1 influenza.

Main Methods:

  • Virtual screening of a fragment-based chemical library against the H1N1 PA endonuclease active site.
  • Experimental validation using crystal violet and MTT assays to determine antiviral activity and cytotoxicity in MDCK cells.

Main Results:

  • A novel triazole-pyridine derivative was identified as a potent inhibitor of the H1N1 PA endonuclease.
  • The compound demonstrated significant antiviral activity with an IC50 of 1.392 μM/mL and a favorable selectivity index (CC2⁽ = 495 μmol/mL).
  • Binding affinity was correlated with specific residue interactions within the PA active site.

Conclusions:

  • The identified triazole-pyridine derivative is a promising lead compound for developing new H1N1 influenza inhibitors.
  • Virtual fragment-based screening is an effective method for discovering novel antiviral agents targeting viral enzymes.
  • This study provides a valuable direction for next-generation influenza therapeutics with improved safety profiles.