β-Carboline ring is one of the most important scaffolds in drug discovery owing to its abundance in nature and its various biological activity. A large number of β-carboline alkaloids were isolated from plants, mammals, marine organisms, fungi and bacteria. Various biological activities have been identified for synthetic β-carboline compounds like anticancer, antimicrobial, antileishmanial, antimalarial, anti-Alzheimer, anti-inflammatory, analgesic and vasorelaxant activity. The present review describes the method of synthesis of β-carboline and highlights the recent progress achieved in the last decade in the development of biologically active β-carboline derivatives.

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生物活性研究进展

β-咔啉环因其在自然界中的丰富性和多种生物活性而成为药物发现中最重要的支架之一。从植物、哺乳动物、海洋生物、真菌和细菌中分离出大量β-咔啉生物碱。合成的 β-咔啉化合物已被鉴定具有多种生物活性，例如抗癌、抗菌、抗地什曼药、抗疟、抗阿尔茨海默病、抗炎、镇痛和血管舒张剂活动。本综述介绍了β-咔啉的合成方法，并重点介绍了过去十年在生物活性物质开发方面取得的最新进展β-咔啉衍生物。