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吡啶并稠合二氮杂卓、恶唑并氮杂卓和噻唑并氮杂卓的合成。

Synthesis of Pyrido-annelated Diazepines, Oxazepines and Thiazepines.

作者信息

Muylaert Koen, Jatczak Martyna, Mangelinckx Sven, Stevens Christian V

机构信息

Department of Sustainable Organic Chemistry and Technology, Campus Coupure, Ghent University, Coupure Links 653, 9000 Ghent, Belgium.

出版信息

Curr Med Chem. 2016;23(42):4784-4823. doi: 10.2174/0929867323666160920101332.

Abstract

The immense amount of research on benzodiazepines resulted in the synthesis of heterocycle-fused diazepine derivatives with potential pharmacological activity. Pyridoazepines are recognized to be active in the central nervous system and have a comparable activity to the well-known benzodiazepines. This makes the synthesis and the study of pyridodiazepines an important research topic. This review comprises of the synthesis and activity of pyridodiazepines, pyridooxazepines and pyridothiazepines. Although these structures have a great similarity with benzodiazepines, much less work has been published on their synthesis or derivatization. Therefore, there is a need to further develop these classes of underexplored scaffolds, in search for new chemistry, new methodology and hence new biological features.

摘要

对苯二氮䓬类药物的大量研究促成了具有潜在药理活性的杂环稠合二氮䓬衍生物的合成。吡啶并二氮䓬类被认为在中枢神经系统中具有活性,且与著名的苯二氮䓬类具有相当的活性。这使得吡啶并二氮䓬类的合成和研究成为一个重要的研究课题。本综述涵盖了吡啶并二氮䓬类、吡啶并恶唑䓬类和吡啶并噻二氮䓬类的合成与活性。尽管这些结构与苯二氮䓬类有很大的相似性,但关于它们的合成或衍生化的研究报道要少得多。因此,有必要进一步开发这些研究较少的支架类别,以寻找新的化学、新的方法,进而获得新的生物学特性。

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