Synthesis and Anti-HBV Activity of Novel Dihydropyrimidine Analogs
Synthesis and Anti-HBV Activity of Novel Dihydropyrimidine Analogs
复制标题
DOI：
10.1360/052011-557
复制
发表时间：
2011-10
期刊：
影响因子：
--
通讯作者：
Zhao Guoming;Wang Xiao-kui;Z. Xuejun;G. Hua;Zhongli Wu;Wang Li-li;Xiao Jun-hai;Y. Xiaohong
中科院分区：
文献类型：
--
作者：
Zhao Guoming;Wang Xiao-kui;Z. Xuejun;G. Hua;Zhongli Wu;Wang Li-li;Xiao Jun-hai;Y. Xiaohong
以芳香腈为原料，经氨解、乙酰化、催化氢化、环合等反应合成了14种新型二氢嘧啶类似物。所有化合物的结构均经1H NMR、MS和元素分析确证，并在转染的HepG2.2.15细胞中进行了抗病毒活性测试。结果表明，部分化合物具有较好的活性。化合物5c和5 n的IC 50分别为0.87和0.67 μmol/L。讨论了2-杂芳基的构效关系，并利用分子排阻色谱研究了活性化合物与衣壳的相互作用。
Fourteen novel dihydropyrimidine analogs were synthesized from aromatic nitriles through ammonolysis, acetylation, catalytic hydrogenation and cyclization procedures. All the compounds were characterized by 1H NMR, MS and elemental analysis and the antiviral activity was tested in transfected HepG2.2.15 cells. The results show that some compounds had effective activity. The IC50 of compounds 5c and 5n were 0.87 and 0.67 μmol/L, respectively. The structure-activity relationship of 2-heteroaryl was discussed and the interaction of active compounds with capsid was studied by size exclusion chromatography.