| 二芳基嘧啶类HIV-1非核苷类逆转录酶抑制剂研究进展 |
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| 引用本文： | 田兴涛,谢蓝. 二芳基嘧啶类HIV-1非核苷类逆转录酶抑制剂研究进展[J]. 药学学报, 2010, 45(2): 177-183 |
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| 作者姓名： | 田兴涛 谢蓝 |
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| 作者单位： | (军事医学科学院毒物药物研究所, 北京 100850) |
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| 基金项目： | 国家自然科学基金资助项目(20472114); 北京市自然科学基金资助项目(7052057) |
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| 摘 要： | 2008年FDA批准上市的新一代非核苷类逆转录酶抑制剂Etravirine (TMC125) 和Ⅲ期临床候选药Rilpivirine (TMC278) 都是二芳基嘧啶 (DAPY) 类化合物, 均对HIV野生型和多种耐药性病毒株有相当强的抑制作用。DAPY类药物的发现和发展是多学科合作研发新药的成功范例。本文综述了新一代HIV非核苷类逆转录酶抑制剂DAPY类化合物的发现、发展及最新研究进展。
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| 关 键 词： | 人类免疫缺陷病毒 非核苷类逆转录酶抑制剂 二芳基嘧啶类化合物 Etravirine Rilpivirine |
Discovery and development of diarylpyrimidines (DAPYs) as next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) |
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| TIAN Xing-tao,XIE Lan. Discovery and development of diarylpyrimidines (DAPYs) as next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)[J]. Acta pharmaceutica Sinica, 2010, 45(2): 177-183 |
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| Authors: | TIAN Xing-tao XIE Lan |
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| Affiliation: | TIAN Xing-tao,XIE Lan (Institute of Pharmacology , Toxicology,Academy of Military Medical Sciences,Beijing 100850,China) |
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| Abstract: | The new HIV-1 NNRTI drug Etravirine (TMC125) and a promising drug candidate Rilpivirine (TMC278) in phase III clinical trial are compounds belonging to the diarylpyrimidine (DAPY) family. They are extremely high potent against both wild-type and many drug-resistant HIV-1 strains, providing new hope for HIV-infected patients who fail to use current drugs due to the emergence of drug-resistant HIV mutants. The discovery and development of DAPY derivatives as next-generation NNRTI drugs depend on multidisciplinary coordination and their success has encouraged new researches to explore more next-generation NNRTIs with new scaffolds. This review described the story of discovery and development of DAPY derivatives as next-generation NNRTIs and related progress. |
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| Keywords: | HIV-1 NNRTI diarylpyrimidine Etravirine Rilpivirine |
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