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Huprines — an insight into the synthesis and biological properties
Russian Chemical Reviews ( IF 7.7 ) Pub Date : 2020-09-18 , DOI: 10.1070/rcr4938
Eva Mezeiova 1, 2 , Ondrej Soukup 1, 2 , Jan Korabecny 1, 2
Affiliation  

The overlapping of tacrine and (–)-huperzine A templates yielded a family of highly potent cholinesterase inhibitors, so-called huprines. A relatively easy access to these compounds led to the development of dozens of huprine derivatives allowing to draw structure – activity relationship mainly for acetylcholinesterase and butyrylcholinesterase enzymes, but also with application to other biological targets of interest. An extension of their pharmacological profile is commonly associated with huprine scaffold binding to some other pharmacophores that yield high-molecular-weight heterodimers. The main purpose in developing the huprine family is related to Alzheimer’s disease therapy. However, these compounds are also interesting lead structures in the treatment of other disorders, such as Myasthenia gravis, African trypanosomiasis, malaria, and prion diseases. The present review provides a rationale behind the development of huprines, detailed synthetic routes leading to different classes of huprines, and a thorough discussion of their potential pharmacological applications.

The bibliography includes 174 references.



中文翻译:

Huprines-对合成和生物学特性的深入了解

他克林和(-)-石杉碱甲模板的重叠产生了一系列高效的胆碱酯酶抑制剂,即所谓的胡派林。相对容易地获得这些化合物导致开发了数十种菊苣碱衍生物,这些衍生物可以画出主要与乙酰胆碱酯酶和丁酰胆碱酯酶有关的构效关系,而且还可以应用于其他感兴趣的生物靶标。它们的药理学特征的扩展通常与虎杖碱支架与产生高分子量异二聚体的一些其他药效团的结合有关。发展人参碱家族的主要目的与阿尔茨海默氏病治疗有关。但是,这些化合物在治疗其他疾病(如重症肌无力,非洲锥虫病,疟疾,和病毒疾病。本综述提供了发展人参碱的理论基础,导致不同种类人参碱的详细合成路线以及对它们潜在药理学应用的详尽讨论。

参考书目包括174种参考文献。

更新日期:2020-09-18
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