Department of Pharmacy, The First Affiliated Hospital, Zhengzhou University, Zhengzhou 450000, China.
Psychology Ward 1, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450000, China.
Curr Med Chem. 2018;25(19):2233-2244. doi: 10.2174/0929867325666171129131311.
Antibiotic resistance is one of the biggest threats to global health today, leading to higher medical costs and increased mortality. Because of the emergence and rapid spread of new resistance mechanisms globally, a growing number of infections are becoming harder to treat as the antibiotics used to treat them become less effective. Therefore, the development of new effective antimicrobial agents is still urgently needed. In last decades, a large number of structurally novel spirooxindoles have been synthesized mainly based on the ylide intermediates generated in situ and further assessed for their antimicrobial activity against different types of bacteria, leading to the discovery of some potent lead compounds with antimicrobial potentials.
The aim of this review to submarize recent advances on the synthesis, structure- activity relationship studies (SARs) and antimicrobial activity of spirooxindoles.
Peer-reviewed research work on spirooxindoles with antimicrobial activity were downloaded from bibliographic databases and analyzed based on their chemoptypes.
50 papers were retrieved from the literature databases, of which 20 papers described the synthesis and antimicrobial activity of spirooxindoles.
This review highlights the importance of spirooxindoles as potential antimicrobial agents. The antimicrobial activity of spirooxindoles against different types of bacteria is less studied, mainly centering on primary antimicrobial assessment, some of these compounds have showed interesting antimicrobial activity. However, the current study is only limited to primary antimicrobial assessment, no detailed modes of action are investigated.
抗生素耐药性是当今全球健康面临的最大威胁之一，导致医疗费用增加和死亡率上升。由于新的耐药机制在全球范围内的出现和迅速传播，用于治疗感染的抗生素的有效性降低，越来越多的感染变得难以治疗。因此，仍然迫切需要开发新的有效的抗菌剂。在过去几十年中，已经合成了大量结构新颖的螺环氧化吲哚，主要基于原位生成的叶立德中间体，并进一步评估了它们对不同类型细菌的抗菌活性，从而发现了一些具有抗菌潜力的有效先导化合物。
本综述旨在概述螺环氧化吲哚的合成、构效关系研究（SARs）和抗菌活性的最新进展。
从文献数据库中下载了具有抗菌活性的螺环氧化吲哚的同行评审研究工作，并根据其化学类型进行了分析。
从文献数据库中检索到 50 篇论文，其中 20 篇描述了螺环氧化吲哚的合成和抗菌活性。
本综述强调了螺环氧化吲哚作为潜在抗菌剂的重要性。螺环氧化吲哚对不同类型细菌的抗菌活性研究较少，主要集中在初步抗菌评估上，其中一些化合物表现出了有趣的抗菌活性。然而，目前的研究仅局限于初步的抗菌评估，没有对作用模式进行详细研究。
