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Next generation quorum sensing inhibitors: Accounts on structure activity relationship studies and biological activities
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-08-29 , DOI: 10.1016/j.bmc.2020.115728
Mahesh S Majik 1 , Umesh B Gawas 2 , Vinod K Mandrekar 3
Affiliation  

Bacterial resistance is a growing threat which represents major scourge throughout the world. The suitable way to control the present critical situation of antimicrobial resistance would be to develop entirely novel strategies to fight antibiotic resistant pathogens such as quorum sensing (QS) inhibitors or its combination with antibiotics. Anti QS agents can eliminate the QS signals and put the barrier in bio-film formation, consequently, bacterial virulence will be reduced without causing drug-resistance to the pathogens. Among the various anti QS agents identified, especially those of natural origin, furanones or acylatedhomoserine lactones (AHLs) are most popular. Semi-synthetic and synthetic inhibitors have shown greatest potential and have inspired chemists to design synthetically modified QS inhibitors with lactone moiety. This review focuses on anti QS agents (bio-film inhibitors) of both natural and synthetic origins. Further, the synthesis, structure activity relationship and anti QS activity covering literature from 2015 till March 2020 has been discussed.



中文翻译:

下一代群体感应抑制剂:关于结构活性关系研究和生物活性的描述

细菌耐药性是一个日益严重的威胁,它代表着全世界的主要祸害。控制当前抗药性的关键情况的合适方法是开发全新的策略来对抗抗生素抗性病原体,例如群体感应(QS)抑制剂或其与抗生素的组合。抗QS剂可以消除QS信号,并在生物膜形成过程中设置障碍,因此,细菌毒力将降低而不会对病原体产生耐药性。在已鉴定的各种抗QS药物中,尤其是天然来源的抗QS药物中,呋喃酮或酰化高丝氨酸内酯(AHLs)最为流行。半合成和合成抑制剂已显示出最大的潜力,并启发了化学家设计具有内酯部分的合成修饰的QS抑制剂。这篇综述着重于天然和合成来源的抗QS试剂(生物膜抑制剂)。此外,还讨论了2015年至2020年3月涵盖文献的合成,结构活性关系和抗QS活性。

更新日期:2020-09-07
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