Anti-HSV activity and mode of action study of alpha-pyrone carboxamides

作者:Karampuri Srinivas; Ojha Durbadal; Bag Paromita; Chakravarty Harapriya; Bal Chandralata; Chattopadhyay Debprasad; Sharon Ashoke*
来源:RSC Advances, 2014, 4(33): 17354-17363.
DOI:10.1039/c4ra01303d

摘要

The clinical management of herpes virus diseases is limited due to ineffective clearance of virus particles and frequent emergence of drug-resistant viruses, particularly in immunocompromised patients, pregnant women and neonates. In our continued quest for new antiviral leads, alpha-pyrone carboxamide propanol derivatives were synthesized and evaluated in HSV infected Vero cells. Compound 3d showed potent antiviral activity against HSV-IF (EC50 = 9.8 mu g ml(-1) and EC99 = 18.0 mu g ml(-1)) and HSV-2G (EC50 = 12.4 mu g ml(-1) and EC99 = 24.0 mu g ml(-1)) at 4-6 h post-infection. The mode of action studies demonstrated that 3d did not interfere in viral attachment or penetration, however, it reduced the expression of ICP4 and ICP27 (immediate-early gene products) as well as the HSV DNA polymerase.

  • 出版日期2014