Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives
文献类型:期刊论文
作者 | Luo, Yu1; Yao, Jia-Ping1; Yang, Li2; Feng, Chun-Lan2; Tang, Wei2![]() ![]() |
刊名 | ARCHIV DER PHARMAZIE
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出版日期 | 2011-02 |
卷号 | 344期号:2页码:78-83 |
关键词 | Anti-HBV Synthesis Thiazolylbenzimidazole |
ISSN号 | 0365-6233 |
DOI | 10.1002/ardp.201000167 |
文献子类 | Article |
英文摘要 | Recently, heterocyclic benzimidazole derivatives have been investigated and validated as a promising class of antiviral agents. In this paper, a series of novel thiazolylbenzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity on the HepG2.2.15 cell line. Afterwards, the preliminary structure-activity relationship (SAR) was discussed. Compound 8b, with IC(50) 1.1 mu M and SI > 90.9, was the most promising compound and could be selected as a benchmark compound for further investigation. |
WOS关键词 | BENZIMIDAZOLE DERIVATIVES ; NS5B POLYMERASE ; IN-VITRO ; INHIBITORS ; IDENTIFICATION ; REPLICATION ; DESIGN ; ACIDS ; VIVO |
资助项目 | National Basic Research Program of China[30701033] ; Shanghai Natural Science Foundation[09ZR1438100] ; State Key Lab of Drug Research of the Chinese Academy of Sciences[SIMM0909 KF-08] |
WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
WOS记录号 | WOS:000287201200002 |
出版者 | WILEY-BLACKWELL |
源URL | [http://119.78.100.183/handle/2S10ELR8/278611] ![]() |
专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
通讯作者 | Lu, Wei |
作者单位 | 1.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; 2.Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China; 3.E China Normal Univ, Inst Drug Discovery & Dev, Shanghai 200062, Peoples R China |
推荐引用方式 GB/T 7714 | Luo, Yu,Yao, Jia-Ping,Yang, Li,et al. Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives[J]. ARCHIV DER PHARMAZIE,2011,344(2):78-83. |
APA | Luo, Yu.,Yao, Jia-Ping.,Yang, Li.,Feng, Chun-Lan.,Tang, Wei.,...&Lu, Wei.(2011).Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives.ARCHIV DER PHARMAZIE,344(2),78-83. |
MLA | Luo, Yu,et al."Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives".ARCHIV DER PHARMAZIE 344.2(2011):78-83. |
入库方式: OAI收割
来源:上海药物研究所
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