期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 162, 期 -, 页码 465-494出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.11.031
关键词
Azepane; Drug discovery; SAR; Biological activities
资金
- Natural Science Foundation of Hubei Province [2014CFB787]
- National Natural Science Foundation of China [21801197]
Azepane-based compounds showed a variety of pharmacological properties, and its derivatives possess a high degree of structural diversity, and it is useful for the discovery of new therapeutic agents. The development of new less toxic, low-cost and highly active azepane-containing analogs is a hot research topic in medicinal chemistry. Now, more than 20 azepane-based drugs have been approved by FDA, and widely used to treat various types of diseases. This review highlights the recent developments of azepane-based compounds in a wide range of therapeutic applications, such as anti-cancer, anti tubercular, anti-Alzheimer's disease, and antimicrobial agents, as well as, histamine H-3 receptor inhibitors, alpha-glucosidase inhibitors, anticonvulsant drugs and other miscellaneous applications. We here briefly describe the structure-activity relationship (SAR) and molecular docking studies of potential bioactive compounds for future discovery of suitable drug candidates. It can serve as an inspiration for new ideas for design and development of less toxic and more powerful azepane-based drugs against numerous devastating diseases. (C) 2018 Elsevier Masson SAS. All rights reserved.
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