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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
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Berberine chloride form
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