Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus
文献类型：期刊论文
| 作者 | Li, Yun-Fei1; Wang, Gui-Feng1 ; Luo, Yu1,2; Huang, Wei-Gang1; Tang, Wei1; Feng, Chun-Lan1; Shi, Li-Ping1; Ren, Yu-Dan1; Zuo, Jian-Ping1; Lu, Wei2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2007-11 |
| 卷号 | 42期号:11-12页码:1358-1364 |
| 关键词 | benzimidazoles synthesis anti-HBV activity |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2007.03.005 |
| 文献子类 | Article |
| 英文摘要 | A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC50 < 4 mu M) with high selectivity indices (SIs > 40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC(50)s of 0.70-2.0 mu M and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC(50)s = 0.70 mu M, SIs > 120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs. (C) 2007 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | REPLICATION ; DERIVATIVES ; INFECTIONS ; LAMIVUDINE ; ENTECAVIR ; ASSAY ; DNA |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000251927500004 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273123]  |
| 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 | Zuo, Jian-Ping |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, SIBS, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.E China Normal Univ, Dept Chem, Shanghai Key Lab Green Chem & Chem Proc, Inst Med Chem, Shanghai 200062, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Yun-Fei,Wang, Gui-Feng,Luo, Yu,et al. Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2007,42(11-12):1358-1364. |
| APA | Li, Yun-Fei.,Wang, Gui-Feng.,Luo, Yu.,Huang, Wei-Gang.,Tang, Wei.,...&Lu, Wei.(2007).Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,42(11-12),1358-1364. |
| MLA | Li, Yun-Fei,et al."Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 42.11-12(2007):1358-1364. |
入库方式： OAI收割
来源：上海药物研究所
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