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Triketones active against antibiotic-resistant bacteria: synthesis, structure-activity relationships, and mode of action |
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| Authors: | van Klink John W Larsen Lesley Perry Nigel B Weavers Rex T Cook Gregory M Bremer Phil J MacKenzie Andrew D Kirikae Teruo |
| Institution: | aNew Zealand Institute for Crop & Food Research Ltd, University of Otago, PO Box 56 Dunedin, New Zealand bDepartment of Chemistry, University of Otago, PO Box 56 Dunedin, New Zealand cDepartment of Microbiology and Immunology, University of Otago, PO Box 56 Dunedin, New Zealand dDepartment of Food Science, University of Otago, PO Box 56 Dunedin, New Zealand eDepartment of Infectious Diseases and Tropical Medicine, Research Institute, International Medical Center of Japan, Tokyo 162-8655, Japan |
| Abstract: | A series of acylated phloroglucinols and triketones was synthesized and tested for activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE) and multi-drug-resistant Mycobacterium tuberculosis (MDR-TB). A tetra-methylated triketone with a C12 side chain was the most active compound (MIC of around 1.0 μg/ml against MRSA) and was shown to stimulate oxygen consumption by resting cell suspensions, suggesting that the primary target was the cytoplasmic membrane. |
| Keywords: | Triketone Phloroglucinol Stucture–activity relations Antibacterial Drug-resistant Membrane Lipophilic |
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