Synthesis of acylphloroglucinols and their antibacterial activities against clinical isolates of MRSA strains

MM Rahman; W Shiu; S Gibbons; JP Malkinson

doi:10.1055/s-0035-1556545

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Planta Med 2015; 81 - PZ1
DOI: 10.1055/s-0035-1556545

Synthesis of acylphloroglucinols and their antibacterial activities against clinical isolates of MRSA strains

MM Rahman ¹^,², W Shiu ¹, S Gibbons ¹, JP Malkinson ¹

¹Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, London WC1N 1AX, UK
²School of Health, Sport and Bioscience, University of East London, London E15 4LZ, UK

Congress Abstract

Bioassay-directed drug discovery efforts on various species of the genus Hypericum led to the discovery of a number of acylphloroglucinols including 4,6-dihydroxy-2-O-(3'',7''-dimethyl-2'',6''-octadienyl)-1-(2'-methylbutanoyl)benzene (6) from H. olympicum with MICs of 0.5 – 1 mg/L against a series of MRSA strains. Its potential activity prompted us to carry out the total synthesis of 6 and its related analogues in order to assess their structure-activity profile as a new group of antibacterial agents. Total synthesis of 6 and a series of structurally related acylphloroglucinols (7-22) as well as their antibacterial activities against a panel of MRSA strains will be presented.