Synthesis of naphtholactams and their biological evaluation against Pseudomonas aeruginosa

The naphtholactam scaffold can be found in a lot of natural products or bioactive compounds, with some previous reports highlighting its antibacterial properties. In this context, we report the synthesis of a library of naphtholactams bearing various functional groups and their biological evaluation against the bacterium Pseudomonas aeruginosa. Their synthesis was accomplished through a concise three-step process, from readily available naphthaldehydes, involving a palladium-catalyzed C8-bromination followed by an oxidation/lactam formation sequence.