抗流感病毒药物神经氨酸酶抑制剂的研究进展  

Advances in anti-influenza drugs:neuraminidase inhibitors

作　　者：田野[1] 杨品[1] 尹志东[2] 周立飞[1] 张振兴[1] 王帅[1] 王鹏[1] 王彬[1] 

机构地区：[1]南开大学药学院,天津300071 [2]延边大学理学院化学系,吉林延吉133002

出　　处：《中国药物化学杂志》2010年第6期531-542,共12页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(20902050);天津市自然科学基金项目(09JCYBJC09200)

摘　　要：由于高致病性禽流感H5N1病毒在亚洲的爆发和H1N1病毒的全球性传播,设计与开发新型抗流感药物尤为迫切。目前,神经氨酸酶(唾液酸苷酶)抑制剂类抗流感药物的研发是整个研究领域的热点。该文回顾了此类上市药物(Relenza和Tamiflu)的发展历程,综述近几年来具有神经氨酸酶抑制活性的化合物和它们的构效关系。对今后新型抑制剂的设计方向提出了建议。The design and development of novel anti-influenza drugs is urgent because of the outbreaks of highly pathogenic avian influenza H5N1 in Asia and worldwide spread of influenza H1N1.At present,reseach and development of anti-influenza drugs based on the inhibition of influenza virus neuraminidase（sialidase） is a very active research area.A historical perspective on the discovery and development of released drugs（Relenza and Tamiflu）,potent compounds with inhibitory activity against neuraminidase and their structure-activity relationships are reviewed.Some suggestions for further design of new inhibitors are also provided herein.

关 键 词：神经氨酸酶抑制剂 唾液酸酶 流感病毒 抗流感药物 构效关系 

分 类 号：R978.7[医药卫生—药品]