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近期六氢喹啉氨基酸及其螺环结构的合成方法及生物学评价。

Recent Synthetic Approaches and Biological Evaluations of Amino Hexahydroquinolines and Their Spirocyclic Structures.

机构信息

Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt.

Chemistry Department (biochemistry branch), Faculty of Science, Cairo University, Giza, Egypt.

出版信息

Anticancer Agents Med Chem. 2019;19(7):875-915. doi: 10.2174/1871520619666190131140436.

Abstract

In this review, the recent synthetic approaches of amino hexahydroquinolines and their spirocyclic structures were highlighted. The synthetic routes include, two-components, three-components or fourcomponents reactions. The two-component [3+3] atom combination reaction represents the simplest method. It involves Michael addition of the electron rich β-carbon of β-enaminones to the activated double bond of cinnamonitriles followed by cyclization to yield hexahydroquinoline compounds. The bioactivity profiles and SAR studies of these compounds were also reviewed with emphasis to the utility of these substances as antimicrobial, anticancer and antitubercular agents, as well as calcium channel modulators.

摘要

在这篇综述中,重点介绍了氨基六氢喹啉及其螺环结构的最新合成方法。这些合成路线包括二组分、三组分或四组分反应。二组分[3+3]原子组合反应是最简单的方法。它涉及β-烯胺酮的富电子β-碳与肉桂腈的活化双键的迈克尔加成,然后环化得到六氢喹啉化合物。还综述了这些化合物的生物活性谱和 SAR 研究,重点介绍了这些物质作为抗菌、抗癌和抗结核药物以及钙通道调节剂的用途。

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