5-(苄硫基)-4-氨甲酰基-1,2,3-三唑对人巨细胞病毒（CMV）和水痘带状疱疹病毒（VZV）的合成及抗病毒活性
Synthesis and Ativiral Activity of 5-(Benzylthio)-4-carbamyl-1,2,3-triazoles Against Human Cytomegalovirus (CMV) and Varicella-zoster Virus (VZV).
作者信息
Wen Yi-Ning, Zhang Zhi-Feng, Liu Ning-Ning, Andrei Graciela, Snoeck Robert, Xiang Yu-Hong, Schols Dominique, Chen Xue, Zhang Zhuo-Yong, Zhang Qing-Shan, Wu Qin-Pei
机构信息
Department of Applied Chemistry and Pharmaceutics, Beijing Institute of Technology, Beijing 100081, China.
Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
出版信息
Med Chem. 2017;13(5):453-464. doi: 10.2174/1573406413666170307165236.
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.
背景
所有用于治疗疱疹病毒感染的临床药物都具有高毒性且耐药性显著。迫切需要开发具有不同作用机制的新型、有效且安全的抗疱疹病毒药物。
方法
高效合成了一系列新型5-（苄硫基）-1H-1,2,3-三唑-4-甲酰胺，并在体外评估了其对人巨细胞病毒（HCMV）、水痘带状疱疹病毒（VZV）和单纯疱疹病毒（HSV）的半数有效浓度（EC50）值。
结果
一些化合物具有抗病毒活性。化合物7f对HCMV和VZV均表现出有前景的抑制活性。我们的结果还表明，这些衍生物的激活不依赖于病毒胸苷激酶（TK），而TK是目前药物所必需的。
结论
4,5-双取代三唑对疱疹病毒有活性，苯环上取代基的性质和位置显著影响其活性，如溴、氰基和氰基乙烯基取代基。未来应开展研究以探究这些化合物的作用机制。
Zotero 插件