The search for novel classes of antibacterial agents is of increasing importance given the emerging resistance seen against the current standards of care in both hospital and community settings.  Toward this end, a high throughput screen for inhibitors of protein synthesis utilizing an E. coli-based transcription-coupled translation (TT) assay coupled to the production of firefly luciferase was undertaken against AstraZeneca's corporate screening deck.  From the screen two series of interest were identified that possessed good inhibitory activity in the TT assay: the phenylisoxazoles and the squaric amides.  This talk will cover the SAR generated for the two series, improvements made to the physical properties of the chemical starting points and discuss target identification work undertaken for the two series.

Novel inhibitors of bacterial protein synthesis identified by high throughput screening

244th National Meeting (2012)

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