| 新型非拟肽磺胺类HIV蛋白酶抑制剂Darunavir的研究进展 |
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| 引用本文： | 郝格非,杨光富.新型非拟肽磺胺类HIV蛋白酶抑制剂Darunavir的研究进展[J].有机化学,2008,28(9):1545-1552. |
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| 作者姓名： | 郝格非 杨光富 |
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| 作者单位： | 华中师范大学化学学院农药与化学生物学教育部重点实验室,武汉,430079 |
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| 摘 要： | 综述新型非拟肽磺胺类人类免疫缺陷病毒(HIV)蛋白酶抑制剂Darunavir (TMC-114)的发现, 抗病毒的活性, 分子模拟以及结构优化的研究进展. Darunavir不但对野生型的HIV蛋白酶有很好的抑制活性, 而且对多种抗性突变的HIV蛋白酶也有良好的活性, 是针对耐药性HIV所开发的新药.
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| 关 键 词： | Darunavir (TMC-114) HIV蛋白酶抑制剂 艾滋病 抗性突变 |
| 收稿时间： | 2007-9-11 |
| 修稿时间： | 2007-12-3 |
Progress in the New Generation Nonpeptide Sulfonamide Anti-HIV Protease Inhibitor Darunavir |
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| HAO, Ge-Fei,YANG, Guang-Fu.Progress in the New Generation Nonpeptide Sulfonamide Anti-HIV Protease Inhibitor Darunavir[J].Chinese Journal of Organic Chemistry,2008,28(9):1545-1552. |
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| Authors: | HAO Ge-Fei YANG Guang-Fu |
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| Institution: | Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, College of Chemistry,
Central China Normal University, Wuhan 430079
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| Abstract: | his article summarizes the discovery, activity, molecular mechanism and structural optimization of nonpeptide sulfonamide anti-HIV (human immunodeficienty virus) protease inhibitor darunavir (TMC-114), which has not only a good inhibitory effect on wildtype HIV protease, but also fantastic inhibitory effects on many mutated HIV proteases, and is a new drug developed for HIV’s resistance. |
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| Keywords: | Darunavir(TMC-114) |
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