Jump to main content
Jump to site search

Issue 4, 2017
Previous Article Next Article

Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

Author affiliations

Abstract

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.

Graphical abstract: Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

Back to tab navigation

Supplementary files

Article information


Submitted
08 Jul 2016
Accepted
25 Jul 2016
First published
27 Jul 2016

Med. Chem. Commun., 2017,8, 720-724
Article type
Research Article

Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

A. T. Garrison, Y. Abouelhassan, H. Yang, H. H. Yousaf, T. J. Nguyen and R. W. Huigens III, Med. Chem. Commun., 2017, 8, 720
DOI: 10.1039/C6MD00381H

Search articles by author

Spotlight

Advertisements