Synthesis and evaluation of antimicrobial activity of new 3-hydroxy-6-methyl-4-oxo-4H-pyran-2-carboxamide derivatives

被引:0
作者
Aytemir, MD [1 ]
Erol, DD
Hider, RC
Özalp, M
机构
[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
[2] Kings Coll London, Dept Pharm, London SE1 8WA, England
[3] Hacettepe Univ, Fac Pharm, Dept Pharmacol Microbiol, TR-06100 Ankara, Turkey
关键词
chlorokojic acid; amide derivatives of pyranone; antibacterial activity; antifungal activity;
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The synthesis of a range of 3-hydroxy-4-oxo-4H-pyran-2-carboxamide with antimicrobial activity is described. Amide derivatives of pyranone were synthesised using TBTU [2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate] as a coupling agent and NMM (N-methylmorpholine) as a base. Antimicrobial activities were determined as MIC values using the microdilution broth method against Staphylococcus aureus, Entrococcus faecalis, Escherichia coli and Pseudomonas aeruginosa for bacteria and Candida albicans, C. krusei and C. parapsilosis for fungi. 3-Hydroxy-6-methyl-4-oxo-4H-pyran-2[N-(4'-methylcoumarin-7-yl)carboxamide] (8c) exhibited higher antibacterial activity against S. aureus, E. faecalis and E. coli than the other compounds. In addition, 8c was more active against C. krusei than the other synthesised compounds.
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页码:757 / 764
页数:8
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