Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives

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• 作者：Zhi-Kun Rao (A1)
  Jing Long (A2)
  Cong Li (A1)
  Sui-Shuan Zhang (A1)
  Mei He (A1)
  Ling-Cheng Ou (A1)
  Yong-Tang Zheng (A2)
  Yan-Ping He (A1)
  
• 关键词：NNRTIs ; S ; DABOs ; Antiviral activity ; HIV ; 1.
• 刊名：Monatshefte f眉r Chemie - Chemical Monthly
• 出版年：2008
• 出版时间：August 2008
• 年：2008
• 卷：139
• 期：8
• 页码：967-974
• 全文大小：309KB
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• 作者单位：Zhi-Kun Rao (A1)
  Jing Long (A2)
  Cong Li (A1)
  Sui-Shuan Zhang (A1)
  Mei He (A1)
  Ling-Cheng Ou (A1)
  Yong-Tang Zheng (A2)
  Yan-Ping He (A1)
  
  A1. Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, People’s Republic of China
  A2. Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Chinese Academy of Sciences, Kunming Institute of Zoology, Kunming, People’s Republic of China
  
• ISSN：1434-4475

文摘

Several 2-heteroaryl-, 2-heteroarylcarbonylmethyl-, 2-arylcarbonylmethyl, and 2-arylethyl derivatives of S-dihydro(alkyloxy)benzyloxypyrimidines have been synthesized and the anti-HIV activities of these compounds were tested in C8166 cell and against RT enzyme. It was found that some of these compounds showed good activity against HIV-1 (EC 50 = 0.014-.8?οem class="a-plus-plus">M) with low toxicity (CC 50 value of 222-64?οem class="a-plus-plus">M) and high selectivity (SI value of 278-7743). The structure-activity relationships (SAR) of these compounds have also been discussed.