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Synthesis, Anti-Varicella-Zoster Virus and Anti-Cytomegalovirus Activity of 4,5-Disubstituted 1,2,3-(1H)-Triazoles

Author(s):

Wei-yuan Yuan, Xue Chen, Ning-ning Liu, Yi-ning Wen, Bei Yang, Graciela Andrei, Robert Snoeck, Yu-hong Xiang, Yong-wei Wu, Zhen Jiang, Dominique Schols, Zhuo-yong Zhang and Qin-pei Wu*   Pages 1 - 12 ( 12 )

Abstract:


Background: Clinical drugs for herpesvirus exhibit high toxicity and suffer from significant drug-resistance. The development of new, effective, and safe anti-herpesvirus agents with different mechanisms of action is greatly required. Objective: Novel inhibitors against herpesvirus with different mechanisms of action from that of clinical drugs. Methods: A series of novel 5-(benzylamino)-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 present antiviral activity. Compounds 5s and 5t are potent against both HCMV and VZV. Compounds 5m, 5n, 5s, and 5t show similar EC50 values against both TK+ and TK- VZV strains. Conclusion: 5-(Benzylamino)-1H-1, 2,3-triazole-4-carboxamides are active against herpesviruses and their activity is remarkably affected by the nature and the position of substituents in the benzene ring. The results indicate that these derivatives are independent of the viral thymidine kinase (TK) for activation, which is indispensable for current drugs. Their mechanisms of action may differ from those of the clinic anti-herpesvirus drugs.

Keywords:

triazole, cytomegalovirus, varicella-zoster virus, antiviral, inhibitor

Affiliation:

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



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