期刊
MEDICINAL CHEMISTRY RESEARCH
卷 27, 期 3, 页码 884-889出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-017-2110-8
关键词
Dehydroacetic acid; Pyran-2, 4-diones; Staphylococcus aureus; SAR; Antibacterial activity
资金
- Division of Pharmacy and Optometry, The University of Manchester
- Presidential Doctoral Scholar award
Dehydroacetic acid is a common pyrone derivative used commercially as an antibacterial and antifungal agent. Based on the synthesis of dehydroacetic acid (1) from N-hydroxysuccinimdyl acetoacetate, a novel series of enamine-based derivatives were synthesised in order to improve the antibacterial activity of dehydroacetic acid. The antibacterial activities of the synthesised analogues were evaluated against Escherichia coli and Staphylococcus aureus. Derivative 4d (N-Ph) was identified as the most potent inhibitor of S. aureus growth. Overall, derivative 4b (N-Me) showed the best broad-spectrum activity with five-fold greater minimum inhibitory concentration and 11-fold greater minimum biocidal concentration against E. coli when compared to dehydroacetic acid, in addition to improved antibacterial activity against S. aureus.
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