Discovery of potent antiviral (HSV-1) quinazolinones and initial structure-activity relationship studies |
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| Authors: | Carla E Brown Tiffany Kong James McNulty Leonardo D&#x;Aiuto Kelly Williamson Lora McClain Paolo Piazza Vishwajit L Nimgaonkar |
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| Institution: | 1. Department of Chemistry & Chemical Biology, McMaster University, Hamilton, Ontario L8S 4M1, Canada;2. Department of Psychiatry, WPIC, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA |
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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. |
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| Keywords: | Quinazolinone Multi component coupling Antiviral HSV-1 Herpesvirus |
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