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  • Title: Antibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group.
    Author: Samosorn S, Tanwirat B, Muhamad N, Casadei G, Tomkiewicz D, Lewis K, Suksamrarn A, Prammananan T, Gornall KC, Beck JL, Bremner JB.
    Journal: Bioorg Med Chem; 2009 Jun 01; 17(11):3866-72. PubMed ID: 19419877.
    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.
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