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Synthesis and antibiofilm evaluation of 3-hydroxy-2,3-dihydroquinazolin-4(1H)-one derivatives against opportunistic pathogen Acinetobacter baumannii.
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-06-29 , DOI: 10.1016/j.bmc.2020.115606 Guo Yang 1 , Cheng Cheng 2 , Guo-Bo Xu 2 , Lei Tang 2 , Kim-Lee Chua 3 , Yuan-Yong Yang 2
中文翻译：
对抗机会病原体鲍曼不动杆菌的3-羟基-2,3-二氢喹唑啉-4（1H）-one衍生物的合成及生物膜评价。
更新日期：2020-07-05
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-06-29 , DOI: 10.1016/j.bmc.2020.115606 Guo Yang 1 , Cheng Cheng 2 , Guo-Bo Xu 2 , Lei Tang 2 , Kim-Lee Chua 3 , Yuan-Yong Yang 2
Affiliation
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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.
中文翻译：
对抗机会病原体鲍曼不动杆菌的3-羟基-2,3-二氢喹唑啉-4（1H）-one衍生物的合成及生物膜评价。
多药耐药性微生物的出现引发了对新的抗微生物策略的迫切需求。具有减轻耐药性的益处的抗病毒策略成为研究的重点。在这项研究中，通过模仿自诱导剂和不动杆菌素的结构合成了22种群体感应抑制剂，在5u时观察到高达34％的生物膜抑制作用。通过胞外多糖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的抑制作用。
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