Efficient discovery of novel antimicrobials through integration of synthesis and testing in crude ribosome extract.

By coupling in situ [ 2+ 3] Huisgen cycloaddition with an in vitro transcription/ translation luminescence assay in a crude ribosomal extract, a robust and accurate high- throughput platform was successfully developed and applied for efficient identification of novel structural types of ribosomal inhibitors with antimicrobial activity against drug- resistant bacteria.