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Early Viral Entry Assays for the Identification and Evaluation of Antiviral Compounds
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Nonpeptide inhibitors of measles virus entry

Aiming Sun1, Andrew Prussia, Weiqiang Zhan

  • 1Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, Georgia 30322, USA.

Journal of Medicinal Chemistry
|August 18, 2006
PubMed

Insights

New anti-measles compounds offer hope against measles virus (MV) infections. Researchers identified potent fusion inhibitors, like AS-48, demonstrating low-micromolar activity against wild-type MV strains.

Area of Science:

  • Virology
  • Medicinal Chemistry

Background:

  • Measles virus (MV) is a highly contagious pathogen responsible for significant mortality and morbidity globally.
  • Existing vaccines, while effective, do not prevent all infections or complications, highlighting the need for antiviral therapies.

Purpose of the Study:

  • To design, synthesize, and evaluate novel nonpeptidic fusion inhibitors targeting the measles virus.
  • To explore the structure-activity relationships (SAR) of identified inhibitor series to guide further optimization.

Main Methods:

  • Utilized a homology model of the MV fusion protein to identify a putative binding site.
  • Designed and synthesized several series of substituted anilides as potential MV fusion inhibitors.
  • Bioevaluated compounds using assays to determine their inhibitory concentration (IC50) against wild-type MV strains.
  • Applied Molecular Field Topology Analysis (MFTA) for quantitative structure-activity relationship (QSAR) analysis.

Main Results:

  • Identified five substituted anilides exhibiting low-micromolar blockade of MV fusion.
  • One compound, AS-48, demonstrated potent activity with IC50 values ranging from 0.6 to 3.0 microM against various wild-type MV strains.
  • MFTA analysis provided insights into structural features correlating with inhibitory potency, suggesting avenues for improvement.

Conclusions:

  • Substituted anilides represent a promising class of nonpeptidic inhibitors for measles virus fusion.
  • The identified lead compound AS-48 shows significant potential for further development as an anti-measles therapeutic.
  • QSAR analysis can effectively guide the rational design of more potent measles virus entry inhibitors.

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