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抗病毒无环核苷膦酸酯的结构活性研究。

Antiviral acyclic nucleoside phosphonates structure activity studies.

作者信息

Holý Antonín

机构信息

Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Centre for Novel Antivirals and Antineoplastics, 166 10 Praha 6, Czech Republic.

出版信息

Antiviral Res. 2006 Sep;71(2-3):248-53. doi: 10.1016/j.antiviral.2006.06.002. Epub 2006 Jun 30.

Abstract

This review concerns acyclic nucleoside phosphonates (ANP) and describes the concept of the design of isopolar and isosteric nucleotide analogues resistant towards degradation by enzymes in vivo. It describes the development of research which led to the discovery of several structurally related potent antivirals and ultimately resulted in the development of drugs directed against HIV, HBV and DNA-virus infections in general, namely adefovir, cidofovir and tenofovir. In addition to these "classical compounds" the review describes the present development in the field of ANP, the "open-ring ANP" and discusses the present achievements, concept of prodrug design and application.

摘要

本综述涉及无环核苷膦酸酯(ANP),并描述了设计对体内酶降解具有抗性的等极性和等电子体核苷酸类似物的概念。它描述了研究的发展历程,该历程导致发现了几种结构相关的强效抗病毒药物,并最终促成了针对HIV、HBV和一般DNA病毒感染的药物的开发,即阿德福韦、西多福韦和替诺福韦。除了这些“经典化合物”,本综述还描述了ANP领域的当前发展,即“开环ANP”,并讨论了当前的成就、前药设计概念和应用。

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