Caged xanthones: Potent inhibitors of global predominant MRSA USA300. Issue 13 (1st July 2016)

• Record Type: Journal Article
• Authors: Chaiyakunvat, Pongkorn; Anantachoke, Natthinee; Reutrakul, Vichai; Jiarpinitnun, Chutima
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 13(2016)
• Page Start: 2980
• Page End: 2983
• Publication Date: 2016-07-01
• Subjects: Caged xanthones -- Methicillin resistant Staphylococcus aureus -- USA300 -- Bacterial invasion; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.05.030
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 12.5 μM). However, its potent toxicity diminishes MRSA therapeutic potential. We synthetically modified natural morellic acid to yield 13 derivatives (3a –3m ). Synthetically modified3b 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.