1,3 - 二取代尿嘧啶对HIV - 1和HCMV的合成及抗病毒活性
Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV.
作者信息
Maruyama Tokumi, Kozai Shigetada, Yamasaki Tetsuo, Witvrouw Myriam, Pannecouque Christophe, Balzarini Jan, Snoeck Robert, Andrei Graciella, De Clercq Erik
机构信息
Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan.
出版信息
Antivir Chem Chemother. 2003 Sep;14(5):271-9. doi: 10.1177/095632020301400506.
The development of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) is an efficient strategy for finding new therapeutic agents against human immunodeficiency virus (HIV). A large number of 6-substituted uracil derivatives have been prepared in order to explore new NNRTIs. However, there are few approaches to anti-HIV agents from 1,3-disubstituted uracil derivatives. Therefore, we tried to prepare several 1,3-disubstituted uracils, which were easily obtainable from uracil by preparation under alkali and Mitsunobu conditions, and examined their antiviral activity against HIV-1 and human cytomegalovirus (HCMV). We found that 1-benzyl-3-(3,5-dimethylbenzyl)uracil and 1-cyanomethyl-3-(3,5-dimethylbenzyl)-4-thiouracil showed powerful inhibition against HCMV and HIV-1, respectively.
开发新型非核苷类逆转录酶抑制剂（NNRTIs）是寻找抗人类免疫缺陷病毒（HIV）新治疗药物的有效策略。为了探索新型NNRTIs，人们已经制备了大量的6-取代尿嘧啶衍生物。然而，从1,3-二取代尿嘧啶衍生物开发抗HIV药物的方法却很少。因此，我们尝试制备了几种1,3-二取代尿嘧啶，它们可通过在碱性条件下和光延反应条件下从尿嘧啶轻松制得，并检测了它们对HIV-1和人巨细胞病毒（HCMV）的抗病毒活性。我们发现1-苄基-3-(3,5-二甲基苄基)尿嘧啶和1-氰甲基-3-(3,5-二甲基苄基)-4-硫尿嘧啶分别对HCMV和HIV-1表现出强大的抑制作用。
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