新型2-芳硫基-5-碘-6-苄基S-DABOs类化合物的合成及作为非核苷类HIV-1 RT抑制剂的活性评估

doi:10.5246/jcps.2012.01.003

新型2-芳硫基-5-碘-6-苄基S-DABOs类化合物的合成及作为非核苷类HIV-1 RT抑制剂的活性评估

张亮, 王孝伟, 刘俊义^*

北京大学医学部药学院化学生物学系, 北京 100191

收稿日期:2011-06-03 修回日期:2011-10-06 出版日期:2012-01-01 发布日期:2012-01-01
通讯作者: 刘俊义*

Synthesis and biological evaluation of novel 2-arylalkylthio-5-iodo-6-benzyl S-DABOs as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

Liang Zhang, Xiao-Wei Wang, Jun-Yi Liu^*

State Key Laboratory of Natural and Biomimetic Drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2011-06-03 Revised:2011-10-06 Online:2012-01-01 Published:2012-01-01
Contact: Jun-Yi Liu*

摘要/Abstract

摘要： 我们设计了一系列新型S-DABOs类目标化合物7a-f, 通过简单有效的方法合成了该系列化合物, 并进行了逆转录酶活性检测, 发现该类化合物具有较好的生物活性, 其中化合物7d的 IC50值达到了3.64 µmol/L, 是Nevirapine的 IC50值的1/2。

关键词: HIV-1逆转录酶, 非核苷类逆转录酶抑制剂, S-DABO类似物

Abstract: A series of novel dihydro-alkylthio-benzyl-oxopyrimidines (S-DABOs) 7a-f have been designed and synthesized with an efficient method. Biological evaluation of their HIV-1 reverse transcriptase inhibitory activities was performed using Nevirapine (NVP) as a reference compound. Among the series, compound 7d shows the highest reverse transcriptase inhibitory activity, which is better than Nevirapine.

Key words: HIV-1 RT, Non-nucleoside reverse transcriptase inhibitors, S-DABOs

中图分类号:

R916

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 20972011, 21042009).
^*Corresponding author. Tel.: 86-10-82805203

张亮, 王孝伟, 刘俊义^*. 新型2-芳硫基-5-碘-6-苄基S-DABOs类化合物的合成及作为非核苷类HIV-1 RT抑制剂的活性评估[J]. , DOI: 10.5246/jcps.2012.01.003.

Liang Zhang, Xiao-Wei Wang, Jun-Yi Liu^* . Synthesis and biological evaluation of novel 2-arylalkylthio-5-iodo-6-benzyl S-DABOs as potent non-nucleoside HIV-1 reverse transcriptase inhibitors [J]. , DOI: 10.5246/jcps.2012.01.003.

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