期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 155, 期 -, 页码 255-262出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.05.038
关键词
Acylphloroglucinols; Total synthesis; Anti-staphylococcal; MRSA
资金
- Heptagon Fund [Heptagon 96/SoP16]
Bioassay-directed drug discovery efforts focusing on various species of the genus Hypericum led to the discovery of a number of new acylphloroglucinols including (S,E)-1-(2-((3,7-dimethylocta-2,6-dien-1-yl) oxy)-4,6-dihydroxyphenyI)-2-methylbutan-1-one (6, olympicin A) from H. olympicum, with MIC5 ranging from 0.5 to 1 mg/L against a series of clinical isolates of multi-drug-resistant (MDR) and methicillinresistant Staphylococcus aureus (MRSA) strains. The promising activity and interesting chemistry of olympicin A prompted us to carry out the total synthesis of 6 and a series of analogues in order to assess their structure-activity profile as a new group of antibacterial agents. Following the synthesis of 6 and structurally-related acylphloroglucinols 7-15 and 18-24, their antibacterial activities against a panel of S. aureus strains were evaluated. The presence of an alkyloxy group consisting of 8-10 carbon atoms ortho to a five-carbon acyl substituent on the phloroglucinol core are important structural features for promising anti-staphylococcal activity. (C) 2018 Elsevier Masson SAS. All rights reserved.
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