Dual inhibition of HCV and HIV by ring-expanded nucleosides containing the 5:7-fused imidazo[4,5-e][1,3]diazepine ring system. In vitro results and implications.
Dual inhibition of HCV and HIV by ring-expanded nucleosides containing the 5:7-fused imidazo[4,5-e][1,3]diazepine ring system. In vitro results and implications.
复制标题
含有 5:7-稠合咪唑并[4,5-e][1,3]二氮杂环系统的扩环核苷对 HCV 和 HIV 具有双重抑制作用。
DOI：
10.1016/j.bmcl.2013.12.121
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发表时间：
2014
影响因子：
2.7
通讯作者：
Hosmane,RamachandraS
中科院分区：
文献类型：
--
作者：
Zhang,Ning;Zhang,Peng;Baier,Andrea;Cova,Lucyna;Hosmane,RamachandraS
以一般结构1和2为代表的扩环核苷(RENS)的例子，在两种细胞培养系统和相应的靶标酶检测中都显示出双重的抗丙型肝炎病毒和抗艾滋病毒活性，包括丙型肝炎病毒NTPase/解旋酶和人RNA解旋酶DDX3。由于丙型肝炎病毒是晚期艾滋病患者的主要混合感染，通常会导致肝硬变和死亡，靶向核苷类似物对丙型肝炎病毒和艾滋病病毒的双重抑制在治疗感染丙型肝炎病毒的艾滋病患者方面具有潜在的有益意义。
Examples of ring-expanded nucleosides (RENs), represented by general structures1and2, exhibited dual anti-HCV and anti-HIV activities in both cell culture systems and the respective target enzyme assays, including HCV NTPase/helicase and human RNA helicase DDX3. Since HCV is a leading co-infection in late stage HIV AIDS patients, often leading to liver cirrhosis and death, the observed dual inhibition of HCV and HIV by the target nucleoside analogues has potentially beneficial implications in treating HIV patients infected with HCV.