Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors.
Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors.
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DOI：
10.1016/j.bmcl.2017.01.010
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发表时间：
2017-02-15
影响因子：
2.7
通讯作者：
Schinazi RF
中科院分区：
文献类型：
--
作者：
Boucle S;Lu X;Bassit L;Ozturk T;Russell OO;Amblard F;Coats SJ;Schinazi RF
探索了对先前报道的HBV衣壳组装效应物如BAY 41-4109、HAP-12和GLS 4的支架的新修饰。已经评估了每种新化合物在HepAD 38系统中的抗HBV活性和细胞毒性特征。其中，五个新的碘-和溴-杂芳基嘧啶类似物显示在低微摩尔范围内的抗HBV活性。
New modifications to the scaffold of previously reported HBV capsid assembly effectors such as BAY 41-4109, HAP-12 and GLS4 were explored. The anti-HBV activity in the HepAD38 system, and cytotoxicity profiles of each of the new compounds has been assessed. Among them, five new iodo- and bromo-heteroarylpyrimidines analogs displayed anti-HBV activity in the low micromolar range.