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  • Antibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group.

Antibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group.

Bioorganic & medicinal chemistry (2009-05-08)
Siritron Samosorn, Bongkot Tanwirat, Nussara Muhamad, Gabriele Casadei, Danuta Tomkiewicz, Kim Lewis, Apichart Suksamrarn, Therdsak Prammananan, Karina C Gornall, Jennifer L Beck, John B Bremner
PMID19419877
ABSTRACT

Conjugation of the NorA substrate berberine and the NorA inhibitor 5-nitro-2-phenyl-1H-indole via a methylene ether linking group gave the 13-substituted berberine-NorA inhibitor hybrid, 3. A series of simpler arylmethyl ether hybrid structures were also synthesized. The hybrid 3 showed excellent antibacterial activity (MIC Staphylococcus aureus, 1.7 microM), which was over 382-fold more active than the parent antibacterial berberine, against this bacterium. This compound was also shown to block the NorA efflux pump in S. aureus.