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Discovery of potent antiviral (HSV-1) quinazolinones and initial structure-activity relationship studies
Carla E Brown1, Tiffany Kong1, James McNulty1
1Department of Chemistry & Chemical Biology, McMaster University, Hamilton, Ontario L8S 4M1, Canada.
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.
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