Title of article :
Triketones active against antibiotic-resistant bacteria: Synthesis, structure–activity relationships, and mode of action Original Research Article
Author/Authors :
John W. van Klink، نويسنده , , Lesley Larsen، نويسنده , , Nigel B. Perry، نويسنده , , Rex T. Weavers، نويسنده , , Gregory M. Cook and Peter Dimroth، نويسنده , , Phil J. Bremer، نويسنده , , Andrew D. MacKenzie، نويسنده , , Teruo Kirikae، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
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
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry