Scientists have recently developed a novel, total synthesis for analogues of Microcin C (McC), a potent antibacterial agent. McC is a Trojan horse inhibitor that is actively taken into sensitive cells and processed to a non-hydrolyzable form that inhibits translation by preventing aminoacylation of tRNAAsp by aspartyl-tRNA synthetase (AspRS). The new synthetic approach results in analogues lacking proplyamine and N-terminal formyl groups, and the phosphoramide normally found in McC is substituted by a sulfamoyl bond. These analogues are taken up by a unique mechanism of action and inhibit aaRS, found in both gram-negative and gram-positive bacteria. These compounds may also be used as coupling agents for other drugs to enhance uptake. Further, synthesis allows for the generation of inhibitors of all 20 aminoacyl-tRNA synthetases and may be widely applicable to creating novel antibiotics.