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

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(英文)

作　　者：Liang Zhang Xiao-Wei Wang Jun-Yi Liu 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)

机构地区：[1]State Key Laboratory of Natural and Biomimetic Drugs,Department of Chemical Biology,School of Pharmaceutical Sciences,Peking University Health Science Center,Beijing 100191,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2012年第1期28-32,共5页中国药学（英文版）

基　　金：National Natural Science Foundation of China (GrantNo.20972011,21042009)

摘　　要：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.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IC_(50)值达到了3.64μmol/L,是Nevirapine的IC_(50)值的1/2。

关 键 词：HIV-1 RT Non-nucleoside reverse transcriptase inhibitors S-DABOs 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]