Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides
文献类型:期刊论文
作者 | Wang Y1; Huang N2,3; Yu X1; Yang LM2; Zhi XY1; Zheng YT[*]2; Xu H[*]1 |
刊名 | MEDICINAL CHEMISTRY
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出版日期 | 2012 |
卷号 | 81期号:5页码:831-833 |
关键词 | Indolyl glyoxamide Acquired immunodeficiency syndrome Human immunodeficiency virus-1 Inhibitor |
通讯作者 | zhengyt@mail.kiz.ac.cn ; orgxuhui@nwsuaf.edu.cn |
合作状况 | 其它 |
英文摘要 | In order to discover compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 9 new indolyl glyoxamide derivatives (3a-i) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among all the derivatives, especially compounds 3e and 3h showed the potent anti-HIV-1 activity with EC50 values of 6.83 and 4.35 mu g/mL, and TI values of >27.15 and 49.45, respectively. It demonstrated that introduction of the substituent R-3 as the halogen atom and the position of R-3 were generally important to their activity. |
收录类别 | SCI |
资助信息 | This work was financially supported in part by grants from New Century Excellent University Talents, State Edu- cation Ministry of China (NCET-06-0868), and the Key Pro- ject of Chinese Ministry of Education (No. 107105). We also would like to acknowledge the National Basic Research Pro- gram of China (2009CB522306), the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029, 2008ZX10005-005), and Scientific and Technological Projects of Yunnan (2007BC006). |
语种 | 英语 |
WOS记录号 | WOS:000309650400008 |
公开日期 | 2013-04-09 |
源URL | [http://159.226.149.42:8088/handle/152453/7310] ![]() |
专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
作者单位 | 1.Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, P. R. China 2.Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, P. R. China 3.Graduate School of the Chinese Academy of Sciences, Beijing 100039, P. R. China |
推荐引用方式 GB/T 7714 | Wang Y,Huang N,Yu X,et al. Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides[J]. MEDICINAL CHEMISTRY,2012,81(5):831-833. |
APA | Wang Y.,Huang N.,Yu X.,Yang LM.,Zhi XY.,...&Xu H[*].(2012).Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides.MEDICINAL CHEMISTRY,81(5),831-833. |
MLA | Wang Y,et al."Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides".MEDICINAL CHEMISTRY 81.5(2012):831-833. |
入库方式: OAI收割
来源:昆明动物研究所
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