title: Synthesis and Ativiral Activity of 5-(Benzylthio)-4-carbamyl-1,2,3-triazoles Against Human Cytomegalovirus (CMV) and Varicella-zoster Virus (VZV).
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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Yi-Ning
authors.initials: YN
authors.lastname: Wen
authors.affiliation: Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Zhi-Feng
authors.initials: ZF
authors.lastname: Zhang
authors.affiliation: Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Ning-Ning
authors.initials: NN
authors.lastname: Liu
authors.affiliation: Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
authors.forename: Graciela
authors.initials: G
authors.lastname: Andrei
authors.affiliation: Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
authors.forename: Robert
authors.initials: R
authors.lastname: Snoeck
authors.affiliation: School of Chemistry, Capital Normal University, Beijing, 100048, China.
authors.forename: Yu-Hong
authors.initials: YH
authors.lastname: Xiang
authors.affiliation: Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
authors.forename: Dominique
authors.initials: D
authors.lastname: Schols
authors.affiliation: Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
authors.forename: Xue
authors.initials: X
authors.lastname: Chen
authors.affiliation: School of Chemistry, Capital Normal University, Beijing, 100048, China.
authors.forename: Zhuo-Yong
authors.initials: ZY
authors.lastname: Zhang
authors.affiliation: Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Qing-Shan
authors.initials: QS
authors.lastname: Zhang
authors.affiliation: Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Qin-Pei
authors.initials: QP
authors.lastname: Wu
mesh_terms: D000212:Acyclovir / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001973:Bromodeoxyuridine / Q000031:analogs & derivatives / Q000494:pharmacology; D000077404:Cidofovir; D003587:Cytomegalovirus / Q000187:drug effects*; D003596:Cytosine / Q000031:analogs & derivatives / Q000494:pharmacology; D015774:Ganciclovir / Q000494:pharmacology; D018259:Herpesvirus 1, Human / Q000187:drug effects; D018258:Herpesvirus 2, Human / Q000187:drug effects; D014645:Herpesvirus 3, Human / Q000187:drug effects*; D063065:Organophosphonates / Q000494:pharmacology; D013937:Thymidine Kinase / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: C000622915:5-(4-bromobenzylthio)-4-(N-phenylcarbamyl)-1H-1,2,3-triazole; D000998:Antiviral Agents; D063065:Organophosphonates; D014230:Triazoles; C020235:brivudine; D003596:Cytosine; D013937:Thymidine Kinase; D001973:Bromodeoxyuridine; D000077404:Cidofovir; D015774:Ganciclovir; D000212:Acyclovir
keywords: Antivirus; cycloaddition; herpes virus; human embryonic lung (HEL); proton derivative; thioether; triazole