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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (9): 1545-1552. 上一篇    下一篇

综述与进展

新型非拟肽磺胺类HIV蛋白酶抑制剂Darunavir的研究进展

郝格非; 杨光富*   

  1. 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
  • 收稿日期:2007-09-11 修回日期:2007-12-03 发布日期:2008-09-20
  • 通讯作者: 杨光富

Progress in the New Generation Nonpeptide Sulfonamide Anti-HIV Protease Inhibitor Darunavir

HAO, Ge-Fei; YANG, Guang-Fu*   

  1. Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, College of Chemistry,
    Central China Normal University, Wuhan 430079
  • Received:2007-09-11 Revised:2007-12-03 Published:2008-09-20
  • Contact: YANG, Guang-Fu

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1881

被引次数

14

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.

关键词: Darunavir (TMC-114), HIV蛋白酶抑制剂, 抗性突变, 艾滋病

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.

Key words: darunavir (TMC-114), acquired immure deficiency syndrome (AIDS), resistant mutati, HIV protease inhibitor