Synthesis of Berberine—Efflux Pump Inhibitor Hybrid Antibacterials

Abstract

This article describes the compact synthesis of two isomeric dual-action hybrid antimicrobials where the 13-position of the antibacterial berberine has been linked via 3′- and 4′-methylene bridges to INF55 (5-nitro-2-phenylindole), an inhibitor of the bacterial NorA multidrug-resistance pump.

Keywords:

• Antibacterial
• 2-arylindole
• berberine
• dual-action
• hybrid
• INF55

ACKNOWLEDGMENTS

We thank the University of Wollongong, Australia, for supporting this work. Award of an NHMRC CJ Martin Fellowship ID252922 to M. Kelso is gratefully acknowledged. This work was supported by NIH grant R01 AI076372.