Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives as a New Class of Potent Dengue Virus Inhibitors
文献类型：期刊论文
| 作者 | Chao, Bo1; Tong, Xian-Kun1 ; Tang, Wei1; Li, De-Wen1; He, Pei-Lan1; Garcia, Jean-Michel2; Zeng, Li-Min1; Gao, An-Hui1; Yang, Li1; Li, Jia1
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| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2012-04-12 |
| 卷号 | 55期号:7页码:3135-3143 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/jm2015952 |
| 文献子类 | Article |
| 英文摘要 | The results of a high-throughput screening assay using the DENV-2 replicon showed that the 2,4-diaminoquinazoline derivative 4a has a high dengue virus inhibitory activity (EC50 = 0.15 mu M). A series of 2,4-diaminoquinazoline derivatives based on 4a as a lead compound were synthesized and subjected to structure-antidengue activity relationship studies. Among the series of 2,4-diaminoquinazoline derivative probed, 4o was observed to display both the highest antiviral potency (EC50 = 2.8 nM, SI > 1000) and an excellent pharmacokinetic profile. |
| WOS关键词 | GONDII DIHYDROFOLATE-REDUCTASE ; SPINAL MUSCULAR-ATROPHY ; BIOLOGICAL EVALUATION ; PNEUMOCYSTIS-CARINII ; LIPOPHILIC INHIBITORS ; STRUCTURE-SELECTIVITY ; ADENOSINE NUCLEOSIDE ; PROTEASE INHIBITORS ; ANTIVIRAL ACTIVITY ; DESIGN |
| 资助项目 | National Science Fair Committee of China[NSFC 81102477] ; State Key Laboratory of Drug Research[SIMM1004KF-18] ; "DENFRAME" of the European Union (EC)[517711] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000302591100023 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278120]  |
| 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 药物化学研究室 |
| 通讯作者 | Zuo, Jian-Ping |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.HKU Pasteur Res Ctr Ltd, Hong Kong, Hong Kong, Peoples R China; 3.Royal Free & Univ Coll Med Sch, London WC1E 6BT, England |
| 推荐引用方式 GB/T 7714 | Chao, Bo,Tong, Xian-Kun,Tang, Wei,et al. Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives as a New Class of Potent Dengue Virus Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2012,55(7):3135-3143. |
| APA | Chao, Bo.,Tong, Xian-Kun.,Tang, Wei.,Li, De-Wen.,He, Pei-Lan.,...&Hu, You-Hong.(2012).Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives as a New Class of Potent Dengue Virus Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,55(7),3135-3143. |
| MLA | Chao, Bo,et al."Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives as a New Class of Potent Dengue Virus Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 55.7(2012):3135-3143. |
入库方式： OAI收割
来源：上海药物研究所
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