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Synthesis and anti-HIV-1 activity evaluation of N-1-alkyl-5-halogeno-6-alkylamino uracils as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
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作者 闫寒 王孝伟 +2 位作者 郭盈 张志丽 刘俊义 《Journal of Chinese Pharmaceutical Sciences》 CAS 2011年第2X期146-153,共8页
N-1-alkyl-5-halogeno-6-alkylamino uracils,which are novel 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues,were synthesized as the selective and potent non-nucleoside human immunodeficiency virus(H... N-1-alkyl-5-halogeno-6-alkylamino uracils,which are novel 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues,were synthesized as the selective and potent non-nucleoside human immunodeficiency virus(HIV)-1 reverse transcriptase inhibitors.Some of the compounds showed potent inhibitory activity against HIV-1 reverse transcriptase.For instance,compounds 1d,1m and 1n exhibited potent anti-HTV-1 activity with the IC_(50) values of 13.3,11.7 and 3.15μM,respectively, which are comparable to that of nevirapine(IC_(50) 8.38μM). 展开更多
关键词 HIV-1 reverse transcriptase Non-nucleoside reverse transcriptase inhibitors hept analogues
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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
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作者 Han Yan Xiao-Wei Wang +2 位作者 Ying Guo Zhi-Li Zhang Jun-Yi Liu 《Journal of Chinese Pharmaceutical Sciences》 CAS 2011年第2期146-153,共8页
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... 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). 展开更多
关键词 HIV-1 reverse transeriptase Non-nucleoside reverse transcriptase inhibitors hept analogues
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