Discovery of potent antiviral (HSV-1) quinazolinones and initial structure-activity relationship studies Journal Articles uri icon

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abstract

  • The discovery of antiviral activity of 2,3-disubstituted quinazolinones, prepared by a one-pot, three-component condensation of isatoic anhydride with amines and aldehydes, against Herpes Simplex Virus (HSV)-1 is reported. Sequential iterative synthesis/antiviral assessment allowed structure-activity relationship (SAR) generation revealing synergistic structural features required for potent anti-HSV-1 activity. The most potent derivatives show greater efficacy than acyclovir against acute HSV-1 infections in neurons and minimal toxicity to the host.

authors

  • Brown, Carla E
  • Kong, Tiffany
  • Mcnulty, James
  • D'Aiuto, Leonardo
  • Williamson, Kelly
  • McClain, Lora
  • Piazza, Paolo
  • Nimgaonkar, Vishwajit L

publication date

  • October 2017