Key Laboratory for Green Chemical Process of Ministry of Education, Hubie Key Laboratory of Novel Reactor and Green Chemical Technology, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 Optics Valley 1st Rd, East Lake New Technology Development District, Wuhan, Hubei, 430205, China; Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, China.
Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, China.
Eur J Med Chem. 2019 Jan 15;162:465-494. doi: 10.1016/j.ejmech.2018.11.031. Epub 2018 Nov 14.
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 receptor inhibitors, α-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.
氮杂环庚烷类化合物具有多种药理学特性,其衍生物具有高度的结构多样性,可用于发现新的治疗剂。开发新型低毒、低成本、高活性的氮杂环庚烷类似物是药物化学的热门研究课题。目前,已有 20 多种基于氮杂环庚烷的药物获得 FDA 批准,并广泛用于治疗各种类型的疾病。本综述重点介绍了氮杂环庚烷类化合物在广泛的治疗应用中的最新进展,如抗癌、抗结核、抗阿尔茨海默病和抗菌药物,以及组胺 H 受体抑制剂、α-葡萄糖苷酶抑制剂、抗惊厥药物和其他杂项应用。我们在这里简要描述了潜在生物活性化合物的结构-活性关系 (SAR) 和分子对接研究,以期为未来发现合适的药物候选物提供启示。这可以为设计和开发针对许多毁灭性疾病的毒性更低、作用更强的氮杂环庚烷类药物提供新的思路。