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.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Garrison AT,Abouelhassan Y,Yang H,Yousaf HH,Nguyen TJ,Huigens Iii RWdoi
10.1039/c6md00381hsubject
Has Abstractpub_date
2016-07-27 00:00:00pages
720-724issue
4eissn
2040-2503issn
2040-2511pii
c6md00381hjournal_volume
8pub_type
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