Journal
CHEMICAL COMMUNICATIONS
Volume 56, Issue 58, Pages 8047-8050Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cc02361b
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Funding
- EPSRC [EP/N025652/1]
- EPSRC [EP/N025652/1] Funding Source: UKRI
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The feasibility of using activity-directed synthesis to drive antibacterial discovery was investigated. An array of 220 Pd-catalysed microscale reactions was executed, and the crude product mixtures were evaluated for activity againstStaphylococcus aureus.Scale-up of the hit reactions, purification and evaluation, enabled expansion of a class of antibacterial quinazolinones. The novel antibacterials had MICs from 0.016 mu g mL(-1)(i.e.38 nM) to 2-4 mu g mL(-1)againstS. aureusATCC29213.
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