摘要
目的设计合成一系列新型1,2,3-三氮唑类化合物,评价其抗人类巨细胞病毒和带状疱疹病毒活性。方法氰基乙酸乙酯与叠氮化物进行环加成反应得到5-氨基-1,2,3-三氮唑类化合物,再与胺类化合物反应将酯基转化为酰胺基得到目标化合物;苯基炔与叠氮化物进行环加成反应得到另外一类1,4-双芳基-1,2,3-三氮唑类目标化合物。测试了部分目标化合物对人类巨细胞病毒(HCMV,AD-169 strain、Davis strain)和水痘-带状疱疹病毒(VZV,TK^+ strain、TK^- strain)的抗病毒活性。结果与结论合成了16个1,2,3-三氮唑类目标化合物,其中,12个是未见文献报道的新化合物。抗病毒活性测试结果显示,化合物4f能够有效地抑制HCMV(EC_(50)=11.7μmol·L^(-1))和VZV(EC_(50)>4μmol·L^(-1))病毒。
Herpes virus is ubiquitous in the world and leads a wide range of diseases. All herpes virus can persist in the organism and establish latent infection after the primary infection. 1,2,3-Triazoles show diverse biological activities including antiviral, anticancer, antifungal and antimycobacteria. Some novel 5-amino-4- carbamyl - 1 - ( 4 -methoxybenzyl ) - 1,2,3 -triazoles and 1,4-diaryl- 1,2,3 -triazoles were efficiently synthesized from benzyl azides via 1,3-dipol cycloaddition and amidation reaction. The antiviral activity against human cytomegalovirus ( HCMV ) and varicella-zoster virus ( VZV ) were evaluated. Compound 4f showed good activity against HCMV with EC50 value of 11.7 μmol-L^-1.
出处
《中国药物化学杂志》
CAS
CSCD
2016年第1期18-23,共6页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(21172019)