Discovery of a series of novel compounds with moderate anti-hepatitis C virus NS3 protease activity in vitro
Discovery of a series of novel compounds with moderate anti-hepatitis C virus NS3 protease activity in vitro
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DOI：
10.1016/j.bmc.2015.07.032
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发表时间：
2015-09-01
影响因子：
3.5
通讯作者：
Xu, Wenfang
中科院分区：
文献类型：
--
作者：
Shi, Fangyuan;Zhang, Yingjie;Xu, Wenfang
丙型肝炎病毒（HCV）NS 3/4A蛋白酶在病毒的生命周期中起着重要作用，已被证明是发现抗HCV药物的良好靶点。受已发现的丙型肝炎病毒NS 3蛋白酶抑制剂β 2-三唑类和酰胺类化合物的启发，我们设计合成了一系列在P1/P1'和P3/P3'位置引入不同氨基酸残基的新型化合物，以开发新型抗病毒药物。酶抑制实验结果表明，所设计的化合物均具有一定的抗HCV NS 3蛋白酶活性。在生物学结果的基础上，推导并讨论了详细的构效关系。(C)2015爱思唯尔有限公司版权所有。
The hepatitis C virus (HCV) NS3/4A protease that plays an important role in the viral life cycle has been proven to be an excellent target for the discovery of anti-HCV drugs. Enlightened by some P2-triazole and amide compounds, which had been found as HCV NS3 protease inhibitors, we designed and synthesized a series of novel compounds by incorporating different amino acid residues in P1/P1' and P3/P3' position to develop novel antiviral agents. The result of enzyme inhibition assay indicated that all the designed compounds showed moderate anti-HCV NS3 protease activity. On the basis of the biological result, a detailed structure-activity relationship (SAR) was derived and discussed. (C) 2015 Elsevier Ltd. All rights reserved.