Synthesis and anti-HIV-1 activity evaluation of N-l-alkyl-5-halogeno-6- alkylamino uracils as novel non-nucleoside HIV-I reverse transcriptase inhibitors  

作　　者：Han Yan Xiao-Wei Wang Ying Guo Zhi-Li Zhang Jun-Yi Liu 

机构地区：[1]Department of Chemical Biology, School of Pharmaceutical Sciences, Peking UniversiOe Health Science Center, Beijing 100191, China [2]State key Laboratory of Natural and Biomimelic Drug, Peking University Health Science Center, Beijing 100191 China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2011年第2期146-153,共8页中国药学（英文版）

基　　金：Foundation items： National Natural Science Foundation of China （Grant No. 20672008 and 20972011）.

摘　　要：N-l-alkyl-5-halogeno-6-alkylamino uracils, which are novel l-[（2-hydroxyethoxy） methyl]-6-（phenylthio） thymine （HEPT） analogues, were synthesized as the selective and potent non-nucleoside human immunodeficiency virus （HIV）-I reverse transcriptase inhibitors. Some of the compounds showed potent inhibitory activity against HIV-1 reverse transcriptase. For instance, compounds ld, lm and In exhibited potent anti-HIV-1 activity with the ICso values of 13.3, 11.7 and 3.15 μM, respectively, which are comparable to that of nevirapine （IC50 8.38 μM）.

关 键 词：HIV-1 reverse transeriptase Non-nucleoside reverse transcriptase inhibitors HEPT analogues 

分 类 号：R916[医药卫生—药学]