摘要
背景:抗生素耐药性是当今全球健康的最大威胁之一,导致医疗费用增加和死亡率上升。由于新的抗蚀剂的出现和迅速扩散在全球范围内,越来越多的感染正在变得越来越难治疗,因为用于治疗它们的抗生素变得不那么有效。因此,开发新的有效的防腐剂仍然迫切需要使用抗生素。在过去的几十年中,合成了大量结构新颖的螺恶吲哚,主要是基于原位生成的YLIDE中间体和A。声称它们对不同类型的细菌具有抗微生物活性,导致发现具有抗微生物电势的一些有效的先导化合物。 目的:综述近年来螺纹酮类化合物的合成、结构活性关系研究(SARS)及抗菌活性的研究进展。 方法:从文献数据库中下载具有抗菌活性的螺氧吲哚类药物的研究成果,并根据其化学类型进行分析。 结果:从文献数据库中检索到50篇文献,其中20篇介绍了螺氧吲哚的合成和抗菌活性。 结论:本综述强调了螺恶吲哚作为潜在的抗菌剂的重要性。对不同类型的细菌对螺环吲哚的抗菌活性研究较少,这些化合物主要集中在初步的抗菌评价上,其中一些化合物显示出有趣的抗菌活性。然而,目前的研究仅限于初级抗菌药物。没有详细的行动模式进行调查。
关键词: 螺环化合物,螺毒素,吲哚,化学合成,抗菌活性,抗真菌活性。
图形摘要
Current Medicinal Chemistry
Title:The Development of Biologically Important Spirooxindoles as New Antimicrobial Agents
Volume: 25 Issue: 19
关键词: 螺环化合物,螺毒素,吲哚,化学合成,抗菌活性,抗真菌活性。
摘要: Background: 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.
Objective: The aim of this review to submarize recent advances on the synthesis, structure- activity relationship studies (SARs) and antimicrobial activity of spirooxindoles.
Methods: Peer-reviewed research work on spirooxindoles with antimicrobial activity were downloaded from bibliographic databases and analyzed based on their chemoptypes.
Results: 50 papers were retrieved from the literature databases, of which 20 papers described the synthesis and antimicrobial activity of spirooxindoles.
Conclusion: 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.
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Cite this article as:
The Development of Biologically Important Spirooxindoles as New Antimicrobial Agents, Current Medicinal Chemistry 2018; 25 (19) . https://dx.doi.org/10.2174/0929867325666171129131311
DOI https://dx.doi.org/10.2174/0929867325666171129131311 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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