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Design, synthesis and biological evaluation of novel unsymmetrical azines as quorum sensing inhibitors

机译：新型非对称吖啶作为批量传感抑制剂的设计，合成及生物学评价

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摘要

Targeting quorum sensing signals using quorum sensing inhibitors has opened new avenues for the application of known antibiotics. In this context, twenty five unsymmetrical azines were synthesised and evaluated as quorum sensing inhibitors. An efficient one-pot procedure was adopted that directly links 3-methyl-2-(methylthio)benzo[d]thiazol-3-ium salt, hydrazine hydrate and substituted aldehyde to give the designed compounds. The synthesized compounds were preliminarily tested for their potential to inhibit CviR receptor based QS signals in Chromobacterium violaceum. The bioassay screening results suggested that two compounds exhibited potent QS inhibition activity against CviR receptor, showing violacein inhibition (>50%) at 200 mu M. Further, the putative positive hits were checked for their potential to inhibit LasR receptor-based QS using the PlasB-gfp(ASV) biomonitor strain of Pseudomonas aeruginosa. These compounds were found to inhibit the QS-mediated GFP signals in a dose dependant manner. Two active compounds also exhibited biofilm clearance at 50 mu M concentration. Docking studies were performed to examine their potential to bind to the LasR protein of Pseudomonas aeruginosa.
机译：使用仲裁感测抑制剂靶向仲裁感测信号已打开新的途径以应用已知的抗生素。在这种情况下，合成了二十五个不对称的吖啶并评估为仲裁感测抑制剂。采用了一种有效的单罐程序，即直接将3-甲基-2-（甲硫基）苯并[D]噻唑-3-Ium盐，肼水合物和取代的醛得到设计，得到设计的化合物。初步测试合成的化合物，以抑制紫杉杆菌基于CVIR受体的QS信号。生物测定筛选结果表明，两种化合物表现出对CVIR受体的有效性QS抑制活性，显示200μmM的紫杉蛋白抑制（> 50％）。此外，检查推定的阳性命令效应抑制基于LASR受体的QS的潜力。使用Pseudomonas铜绿假单胞菌的血浆-GFP（ASV）生物监测菌株。发现这些化合物以剂量依赖性方式抑制QS介导的GFP信号。两种活性化合物还在50μm浓度下表现出生物膜间隙。进行对接研究以检查它们与铜绿假单胞菌的LASR蛋白结合的潜力。

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