摘要
本文按时间顺序讨论了药物设计在抗甲型H1N1流感M2离子通道抑制剂、神经氨酸酶(NA)、血凝素(HA)和RNA依赖的RNA聚合酶复合物(RdRp)靶点开发利用中的应用。除了寻找有效对抗甲型流感(H1N1)新靶点的化学型,我们还对有效药物的优化类似物进行了探寻,同时也讨论了现有抗病毒药物新出现的耐药机制。以突出进一步化学修饰的结构要求,本文对计算研究也进行了总结。
关键词: 甲型流感(H1N1)病毒,药物设计,M2离子通道阻滞剂,HA抑制剂,NA抑制剂,RNA聚合酶复合体抑制剂。
Current Medicinal Chemistry
Title:Fight Against H1N1 Influenza A Virus: Recent Insights Towards the Development of Druggable Compounds
Volume: 23 Issue: 18
Author(s): Michele Tonelli and Elena Cichero
Affiliation:
关键词: 甲型流感(H1N1)病毒,药物设计,M2离子通道阻滞剂,HA抑制剂,NA抑制剂,RNA聚合酶复合体抑制剂。
摘要: In this review we discuss drug design strategies directed to the development of potential anti-influenza A(H1N1) inhibitors of M2 ion channel, neuraminidase (NA), hemagglutinin (HA) and RNA-dependent RNA-polymerase complex (RdRp) major targets, following temporal chronology of their findings. Besides searching for new chemotypes, eventually active against new targets of influenza A (H1N1), the design of optimized analogues of proven drugs is largely pursued, taking into account the emerging insight into the mechanisms of resistance to existing antivirals. Computational studies are also summarized, in order to highlight the structural requirements for further chemical optimizations.
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Cite this article as:
Michele Tonelli and Elena Cichero , Fight Against H1N1 Influenza A Virus: Recent Insights Towards the Development of Druggable Compounds, Current Medicinal Chemistry 2016; 23 (18) . https://dx.doi.org/10.2174/0929867323666160210124930
DOI https://dx.doi.org/10.2174/0929867323666160210124930 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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