With antibacterial resistance becoming an ever increasing problem, the discovery of new biologically active compounds has become an uphill battle. We have synthesized and analyzed the antimicrobial properties of a set of 2,4-diaminoquinazoline analogues. These compounds have been found to be effective against Methicillin Resistant Staphylococcus aureus (MRSA) with the most active compounds having minimum inhibitory concentrations (MIC) < 1 �M. Gene sequencing of the few mutants which were formed using the most active compounds allowed the determination that the mechanism of action for these compounds is not topoisomerase, gyrase, or dihydrofolate reductase inhibition. The synthesis, structure-property relationships and structure-activity relationships are described.

2,4-Diaminoquinazolines as antibacterials

243rd National Meeting (2012)

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