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Title: | Antibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group |
Authors: | Samosorn S. Tanwirat B. Muhamad N. Casadei G. Tomkiewicz D. Lewis K. Suksamrarn A. Prammananan T. Gornall K.C. Beck J.L. Bremner J.B. |
Keywords: | 5 nitro 2 phenyl 1h indole 9,10 dimethoxy 13 [2 (5 nitro 1h indol 2 yl)benzyloxy] 5,6 dihydrobenzo[g] 1,3 benzodioxolo[5,6 a]quinolizinium bromide berberine berberine 5 nitro 2 phenyl 1h indole conjugate inf 55 NorA pump inhibitor protein inhibitor unclassified drug antibacterial activity article bacterial strain controlled study drug conjugation drug potency drug structure drug synthesis minimum inhibitory concentration nonhuman Staphylococcus aureus Anti-Bacterial Agents Bacterial Proteins Berberine Enterococcus faecalis Ether, Ethyl Indoles Intercalating Agents Molecular Structure Multidrug Resistance-Associated Proteins Staphylococcus aureus Bacteria (microorganisms) Staphylococcus aureus |
Issue Date: | 2009 |
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 μM), 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. © 2009 Elsevier Ltd. |
URI: | https://ir.swu.ac.th/jspui/handle/123456789/15176 https://www.scopus.com/inward/record.uri?eid=2-s2.0-65549100031&doi=10.1016%2fj.bmc.2009.04.028&partnerID=40&md5=7d9a30a9bf253d6997e94fd82643d982 |
ISSN: | 9680896 |
Appears in Collections: | Scopus 1983-2021 |
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