摘要/Abstract

开环膦酸核苷类（Acyclic nucleoside phosphonates，ANPs）抗病毒药物在临床上的广泛应用使其越来越受到关注.但其结构中的游离电荷使其生物利用度较低，毒性较大，特别在治疗乙肝或艾滋病毒感染时需要长期用药，其毒性更加不可忽视.将开环膦酸核苷类抗病毒药制备成适当形式的前药，可以使其顺利吸收并在靶部位释放出原药，大幅提高生物利用度，降低毒副作用.以替诺福韦、阿德福韦和西多福韦的结构出发，综述了近几年开环膦酸核苷类前药的研究和应用近况.
关键词: 开环膦酸核苷类, 抗病毒药, 前药
More and more attention has been focused on acyclic nucleoside phosphonates (ANPs) antiviral agents which were wildly used in clinical therapy. However, poor oral bioavailability and high toxicity directly related to the phosphonate charge were serious and unnegligible especially for the treatment of chronic diseases such as hepatitis B virus (HBV) and human immunodeficiency virus (HIV). Preparing appropriate forms of prodrug could enhance the oral bioavailability and reduce the toxicity because of the smooth absorption of prodrugs and the release of active drug only at the target. This review summarizes some recent progress in prodrugs of ANPs antiviral agents based on the structures of tenofovir, adefovir and cidofovir.
Key words: acyclic nucleoside phosphonates (ANPs), antiviral agents, prodrug


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