Synthesis and Structure-Activity Relationships of Imidazole-Coumarin Conjugates against Hepatitis C Virus.
Synthesis and Structure-Activity Relationships of Imidazole-Coumarin Conjugates against Hepatitis C Virus.
复制标题
DOI：
10.3390/molecules21020228
复制
发表时间：
2016-02-18
期刊：
影响因子：
--
通讯作者：
Neyts J
中科院分区：
文献类型：
--
作者：
Tsay SC;Lin SY;Huang WC;Hsu MH;Hwang KC;Lin CC;Horng JC;Chen IC;Hwu JR;Shieh FK;Leyssen P;Neyts J
以咪唑和香豆素衍生物为原料，采用化学方法合成了一系列新的- sch2 -键共轭化合物。实验结果表明，新合成的20种咪唑-香豆素偶联物中，有3种具有较好的EC50值（5.1 ~ 8.4 μM）和抗丙型肝炎病毒选择性指标bbb20。通过两个因素修饰它们的结构，咪唑核在N(1)位置上加一个氢原子，香豆素核在Cl、F、Br、Me和OMe等取代基上加一个取代基，它们的效力和选择性大大提高。这些指南为进一步开发作为抗病毒药物的缀合化合物提供了有价值的信息。
A series of new conjugated compounds with a –SCH2– linkage were synthesized by chemical methods from imidazole and coumarin derivatives. The experimental results indicate that of the twenty newly synthesized imidazole–coumarin conjugates, three of them exhibited appealing EC50 values (5.1–8.4 μM) and selective indices >20 against hepatitis C virus. Their potency and selectivity were increased substantially by modification of their structure with two factors: imidazole nucleus with a hydrogen atom at the N(1) position and coumarin nucleus with a substituent, such as Cl, F, Br, Me, and OMe. These guidelines provide valuable information for further development of conjugated compounds as anti-viral agents.
登录
查看更多内容
影响因子：
9
作者：
Liaudet, L;Mabley, JG;Szabó, C
通讯作者：
Szabó, C
影响因子：
14.9
作者：
Bhan, P;Bhan, A;Hoke, GD
通讯作者：
Hoke, GD
影响因子：
2.8
作者：
Chávez-Gil, TE;Meléndez, E
通讯作者：
Meléndez, E
影响因子：
7.3
作者：
LIN, TS;CHENG, JC;SARTORELLI, AC
通讯作者：
SARTORELLI, AC
影响因子：
4.9
作者：
Hulskotte, E. G. J.;Feng, H. -P.;Butterton, J. R.
通讯作者：
Butterton, J. R.