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Synthesis and Ativiral Activity of 5-(Benzylthio)-4-carbamyl-1,2,3-triazoles Against Human Cytomegalovirus (CMV) and Varicella-zoster Virus (VZV)

[ Vol. 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*   Pages 453 - 464 ( 12 )

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.

Keywords:

Antivirus, cycloaddition, herpes virus, human embryonic lung (HEL), proton derivative, thioether, triazole.

Affiliation:

Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, School of Chemistry, Capital Normal University, Beijing, 100048, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, School of Chemistry, Capital Normal University, Beijing, 100048, Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081

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