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Antibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group
Siritron Samosorn1, Bongkot Tanwirat, Nussara Muhamad
1Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok 10110, Thailand. siritron@swu.ac.th
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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