开环膦酸核苷类抗病毒药物前药的研究进展

doi:10.6023/cjoc201808018

有机化学 ›› 2019, Vol. 39 ›› Issue (4): 974-981.DOI: 10.6023/cjoc201808018 上一篇下一篇

综述与进展

开环膦酸核苷类抗病毒药物前药的研究进展

高梦远^a, 刘洪涛^b, 连玉菲^b, 高欣丰^a, 耿云鹤^a, 李文燕^a

a 河北师范大学化学与材料科学学院石家庄 050024;
b 河北省人民医院药学部石家庄 050051

收稿日期:2018-08-16 修回日期:2018-10-15 发布日期:2018-11-30
通讯作者: 李文燕 E-mail:liyan8512@163.com
基金资助:
河北省自然科学基金（No.H2018307055）、河北师范大学技术创新基金（No.L2017K06）资助项目.

Research Progress in Prodrugs of Acyclic Nucleoside Phosphonates Antiviral Agents

Gao Mengyuana^a, Liu Hongtaob^b, Lian Yufeib^b, Gao Xinfenga^a, Geng Yunhea^a, Li Wenyan^a

a Hebei Normal University, College of Chemistry & Material Science, Shijiazhuang 050024;
b Department of Pharmacy, Hebei General Hospital, Shijiazhuang 050051

Received:2018-08-16 Revised:2018-10-15 Published:2018-11-30
Contact: 10.6023/cjoc201808018 E-mail:liyan8512@163.com
Supported by:
Project supported by the Natural Science Foundation of Hebei Province (No.H2018307055) and the Technology Innovation Foundation of Hebei Normal University (No.L2017K06).

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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

引用此文

高梦远, 刘洪涛, 连玉菲, 高欣丰, 耿云鹤, 李文燕. 开环膦酸核苷类抗病毒药物前药的研究进展[J]. 有机化学, 2019, 39(4): 974-981.

Gao Mengyuana, Liu Hongtaob, Lian Yufeib, Gao Xinfenga, Geng Yunhea, Li Wenyan. Research Progress in Prodrugs of Acyclic Nucleoside Phosphonates Antiviral Agents[J]. Chin. J. Org. Chem., 2019, 39(4): 974-981.

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开环膦酸核苷类抗病毒药物前药的研究进展

Research Progress in Prodrugs of Acyclic Nucleoside Phosphonates Antiviral Agents

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