当前位置: X-MOL 学术Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and Ativiral Activity of 5-(Benzylthio)-4-carbamyl-1,2,3-triazoles Against Human Cytomegalovirus (CMV) and Varicella-zoster Virus (VZV)
Medicinal Chemistry ( IF 1.9 ) Pub Date : 2017-07-31 , DOI: 10.2174/1573406413666170307165236
Yi-ning Wen 1 , Zhi-feng Zhang 1 , Ning-Ning Liu 1 , Graciela Andrei 2 , Robert Snoeck 3 , Yu-Hong Xiang 4 , Dominique Schols 2 , Xue Chen 2 , Zhuo-Yong Zhang 4 , Qing-Shan Zhang 1 , Qin-Pei Wu 1
Affiliation  

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.



中文翻译:

5-(苄硫基)-4-氨基甲酰基1,2,3-三唑类化合物的合成及其抗人巨细胞病毒和水痘带状疱疹病毒的抗病毒活性

背景:所有用于疱疹病毒感染的临床药物均显示高毒性,并具有明显的耐药性。迫切需要开发具有不同作用机制的新型,有效和安全的抗疱疹病毒药物。

方法:有效合成了一系列新型的5-(苄硫基)-1H-1,2,3-三唑-4-羧酰胺,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)在体外进行了评估。

结果:某些化合物具有抗病毒活性。化合物7f对HCMV和VZV均显示出有希望的抑制活性。我们的结果还表明,这些衍生物与病毒胸苷激酶(TK)的激活无关,这对于当前的药物而言是必不可少的。

结论:4,5-双取代的三唑类对疱疹病毒有活性,苯环中取代基的性质和位置显着影响其活性,如溴,氰基和氰基腈取代基。应该进行进一步的研究以研究这些化合物的作用机理。

更新日期:2017-07-31
down
wechat
bug