Title:Synthesis and Ativiral Activity of 5-(Benzylthio)-4-carbamyl-1,2,3-triazoles Against Human Cytomegalovirus (CMV) and Varicella-zoster Virus (VZV)
Volume: 13
Issue: 5
Author(s): Yi-ning Wen, Zhi-feng Zhang, Ning-Ning Liu, Graciela Andrei, Robert Snoeck, Yu-Hong Xiang, Dominique Schols, Xue Chen, Zhuo-Yong Zhang, Qing-Shan Zhang and Qin-Pei Wu*
Affiliation:
- Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081,China
Keywords:
Antivirus, cycloaddition, herpes virus, human embryonic lung (HEL), proton derivative, thioether, triazole.
Abstract: Background: All of the clinical drugs for herpesvirus infections exhibit high toxicity
and suffer from significant drug-resistantance. There is a great need for the development of new,
effective, and safe anti-herpesvirus agents with different mechanisms of action.
Methods: A series of novel 5-(benzylthio)-1H-1,2,3-triazole-4-carboxamides were efficiently synthesized
and EC50 values against human cytomegalovirus (HCMV), varicella-zoster virus (VZV)
and herpes simplex virus (HSV) were evaluated in vitro.
Results: Some compounds possess antiviral activity. Compound 7f exhibits promising inhibitory
activity against both HCMV and VZV. Our results also indicate that these derivatives are independent
of the viral thymidine kinase (TK) for activation, which is indispensable for current drugs.
Conclusion: 4,5-Bissubstiuted triazoles are active against herpesviruses and the nature and the position
of substituents in the benzene ring remarkably affect their activity, such as bromo, cyano
and cyanovynil substituents. Future studies should be undertaken to investigate the mechanism of
action of these compounds.