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合成及 3-羟基-2,3-二氢喹唑啉-4(1H)-酮衍生物对机会性病原体鲍曼不动杆菌的抗生物膜活性评价。

Synthesis and antibiofilm evaluation of 3-hydroxy-2,3-dihydroquinazolin-4(1H)-one derivatives against opportunistic pathogen Acinetobacter baumannii.

机构信息

State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China; The Second People's Hospital of Guizhou Province, Department of Pharmacy, Guiyang 550004, China.

State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China.

出版信息

Bioorg Med Chem. 2020 Aug 15;28(16):115606. doi: 10.1016/j.bmc.2020.115606. Epub 2020 Jun 29.

Abstract

The emergence of multidrug resistant microorganisms has triggered the impending need for new aitimicrobial strategies. The antivirulence strategy with the benefite of alleviating the drug resistance becomes the focus of research. In this study, 22 quorum sensing inhibitors were synthesized by mimicking the structure of autoinducer and acinetobactin and up to 34% biofilm inhibition was observed with 5u. The biofilm inhibition effect was further demonstrated with extracellular polysaccharides inhibition and synergism with Gentamycin sulphate.

摘要

多药耐药微生物的出现引发了对抗生素策略的新需求。具有缓解耐药性优势的抗毒力策略成为研究的焦点。在这项研究中,通过模拟自动诱导物和不动菌素的结构合成了 22 种群体感应抑制剂,其中 5u 观察到高达 34%的生物膜抑制作用。通过对胞外多糖的抑制作用和与硫酸庆大霉素的协同作用进一步证明了生物膜抑制作用。

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