期刊
MOLECULES
卷 25, 期 10, 页码 -出版社
MDPI
DOI: 10.3390/molecules25102405
关键词
xanthones; diversity-oriented synthesis; antifungal activity; antibacterial activity
资金
- FCT (Foundation for Science and Technology) [UIDB/04423/2020, UIDP/04423/2020, PTDC/SAU-PUB/28736/2017, POCI-01-0145-FEDER-028736]
- COMPETE 2020 through the ERDF
- Portugal 2020 through the ERDF
- European Union through the ERDF
- FCT [SFRH/BD/135852/2018]
- MDPI
- [CHIRALBIOACTIVE-PI-3RL-IINFACTS-2019]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/135852/2018] Funding Source: FCT
A series of thirteen xanthones 3-15 was prepared based on substitutional (appendage) diversity reactions. The series was structurally characterized based on their spectral data and HRMS, and the structures of xanthone derivatives 1, 7, and 8 were determined by single-crystal X-ray diffraction. This series, along with an in-house series of aminated xanthones 16-33, was tested for in-vitro antimicrobial activity against seven bacterial (including two multidrug-resistant) strains and five fungal strains. 1-(Dibromomethyl)-3,4-dimethoxy-9H-xanthen-9-one (7) and 1-(dibromomethyl)-3,4,6-trimethoxy-9H-xanthen-9-one (8) exhibited antibacterial activity against all tested strains. In addition, 3,4-dihydroxy-1-methyl-9H-xanthen-9-one (3) revealed a potent inhibitory effect on the growth of dermatophyte clinical strains (T. rubrum FF5, M. canis FF1 and E. floccosum FF9), with a MIC of 16 mu g/mL for all the tested strains. Compounds 3 and 26 showed a potent inhibitory effect on two C. albicans virulence factors: germ tube and biofilm formation.
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