Herein, we disclose the development of a catalyst- and protecting-group-free microwave-enhanced Friedländer synthesis which permits the single-step, convergent assembly of diverse 8-hydroxyquinolines with greatly improved reaction yields over traditional oil bath heating (increased from 34% to 72%). This rapid synthesis permitted the discovery of novel biofilm-eradicating halogenated quinolines (MBECs = 1.0-23.5 μM) active against MRSA, MRSE, and VRE. These small molecules exhibit activity through mechanisms independent of membrane lysis, further demonstrating their potential as a clinically useful treatment option against persistent biofilm-associated infections.

中文翻译：

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微波增强的Friedländer合成法可快速组装卤化喹啉，并具有针对耐药性和耐受性细菌的抗菌和生物膜清除活性。

本文中，我们公开了无催化剂和无保护基团的微波增强Friedländer合成技术的开发，该技术可实现多种8-羟基喹啉的一步聚合收敛，与传统油浴加热相比，反应产率大大提高（从34％提高到至72％）。这种快速合成使得发现了对MRSA，MRSE和VRE具有活性的新型生物膜消除卤代喹啉（MBEC = 1.0-23.5μM）。这些小分子通过独立于膜裂解的机制表现出活性，进一步证明了其作为针对持久性生物膜相关感染的临床有用治疗选择的潜力。