Non-nucleoside inhibitors of the hepatitis C virus NS5B RNA-dependant RNA polymerase: 2-aryl-3-heteroaryl-1,3-thiazolidin-4-one derivatives.
Non-nucleoside inhibitors of the hepatitis C virus NS5B RNA-dependant RNA polymerase: 2-aryl-3-heteroaryl-1,3-thiazolidin-4-one derivatives.
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丙型肝炎病毒 NS5B RNA 依赖性 RNA 聚合酶的非核苷抑制剂：2-芳基-3-杂芳基-1,3-噻唑烷-4-酮衍生物。
DOI：
10.1016/j.bmcl.2008.10.023
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发表时间：
2008
影响因子：
2.7
通讯作者：
Pan,Zhenhua
中科院分区：
文献类型：
--
作者：
Rawal,RavindraK;Katti,SB;Kaushik-Basu,Neerja;Arora,Payal;Pan,Zhenhua
丙型肝炎病毒（HCV）NS 5 B RNA聚合酶是复制HCV RNA基因组的关键，是开发抗HCV药物的一个有吸引力的目标。评价了一系列新的2，3-二芳基-1，3-噻唑烷-4-酮衍生物抑制HCV NS 5 B的能力。在这一系列中，化合物4c、5 b、5c和6表现出更有效的，在体外显示出超过95%的NS 5 B RNA聚合酶活性抑制。两个活性最高的化合物4c和5c对HCV NS 5 B的IC 50分别为31.9μM和32.2μM。
Hepatitis C virus (HCV) NS5B RNA polymerase is crucial for replicating the HCV RNA genome and is an attractive target for developing anti-HCV drugs. A novel series of 2,3-diaryl-1,3-thiazolidin-4-one derivatives were evaluated for their ability to inhibit HCV NS5B. Of this series, compounds 4c, 5b, 5c and 6 emerged as more potent, displaying over 95% inhibition of NS5B RNA polymerase activity in vitro. The two most active compounds 4c and 5c exhibited an IC50of 31.9μM and 32.2μM, respectively, against HCV NS5B.