2. Academic Validation
  3. Caged xanthones: Potent inhibitors of global predominant MRSA USA300

Caged xanthones: Potent inhibitors of global predominant MRSA USA300

  • Bioorg Med Chem Lett. 2016 Jul 1;26(13):2980-2983. doi: 10.1016/j.bmcl.2016.05.030.
Pongkorn Chaiyakunvat 1,  Natthinee Anantachoke 2,  Vichai Reutrakul 1,  Chutima Jiarpinitnun 1
Affiliations

Affiliations

  • 1 Department of Chemistry and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Mahidol University, Rama VI Road, Bangkok 10400, Thailand.
  • 2 Department of Pharmacognosy and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Pharmacy, Mahidol University, Sri-Ayudhaya Road, Bangkok 10400, Thailand.
PMID: 27216998 DOI: 10.1016/j.bmcl.2016.05.030
Abstract

Total of 22 caged Xanthones were subjected to susceptibility testing of global epidemic MRSA USA300. Natural morellic acid showed the strongest potency (MIC of 12.5μM). However, its potent toxicity diminishes MRSA therapeutic potential. We synthetically modified natural morellic acid to yield 13 derivatives (3a-3m). Synthetically modified 3b retained strong potency in MRSA growth inhibition, yet the toxicity was 20-fold less than natural morellic acid, permitting the possibility of using caged Xanthones for MRSA therapeutic.

Keywords

Bacterial invasion; Caged xanthones; Methicillin resistant Staphylococcus aureus; USA300.

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