| Literature DB >> 19419877 |
Siritron Samosorn1, 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.Entities:
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Year: 2009 PMID： 19419877 PMCID： PMC2759347 DOI： 10.1016/j.bmc.2009.04.028
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641