Institut de Biotecnologia i de Biomedicina, Universitat Autònoma de Barcelona, 08193, Barcelona, Spain.
Departament de Genètica i de Microbiologia, Universitat Autònoma de Barcelona, 08193, Barcelona, Spain.
Future Med Chem. 2019 Jul;11(13):1565-1582. doi: 10.4155/fmc-2019-0015.
() and complex (BCC) are Gram-negative bacterial pathogens, which are typically multidrug resistant and excellent biofilm producers. These phenotypes are controlled by quorum sensing (QS) systems from the diffusible signal factor (DSF) family. We aim to interfere with this QS system as an alternative approach in combatting such difficult-to-treat infections. A library of sulfonamide-based DSF bioisosteres was synthesized and tested against the major phenotypes regulated by QS. Several analogs display significant antibiofilm activity while the majority increase the action of the last-resort antibiotic colistin against and BCC. Most compounds inhibit DSF synthesis in the K279a strain. Our results support the strategy of interfering with QS communications to combat multidrug resistance.
() 和 复杂 (BCC) 是革兰氏阴性细菌病原体，通常具有多重耐药性和出色的生物膜生成能力。这些表型受群体感应 (QS) 系统控制，来自可扩散信号因子 (DSF) 家族。我们旨在干扰这种 QS 系统，作为对抗这种难以治疗的感染的一种替代方法。 我们合成了基于磺胺的 DSF 生物等排体文库，并对受 QS 调节的主要表型进行了测试。 几种类似物显示出显著的抗生物膜活性，而大多数类似物增加了最后手段抗生素粘菌素对 和 BCC 的作用。大多数化合物抑制 K279a 菌株中的 DSF 合成。我们的结果支持干扰 QS 通讯以对抗多药耐药性的策略。
