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.
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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TIAN Xin-Chao, XIE La. Discovery and development of diarylpyrimidines (DAPYs) as next- generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)J. 药学学报, 2010,45(2): 177-183.
Citation: TIAN Xin-Chao, XIE La. Discovery and development of diarylpyrimidines (DAPYs) as next- generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)J. 药学学报, 2010,45(2): 177-183.
shu

二芳基嘧啶类HIV-1非核苷类逆转录酶抑制剂研究进展

Discovery and development of diarylpyrimidines (DAPYs) as next- generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)

    摘要
  • 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。

     

    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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