4-羟基-2(1H)-吡啶酮-3-甲酰胺类冬青生菌素类似物的合成与生物活性

Synthesis and bioactivity of 4-hydroxy-2(1H)-pyridone-3-carboxamide derivatives

以反式-4-羟基肉桂酸为起始原料,经乙酰化、酰基叠氮、curtius重排、加成和环合等6步反应合成了4-羟基-2(1 H)-吡啶酮-3-甲酰胺类冬青生菌素类似物,总收率17%.随后用滤纸片扩散法对该化合物的抑菌性能进行了初步研究.实验表明,该化合物对于白色念珠菌具有较好的抑制作用,对于酵母菌抑制作用较弱,对大肠杆菌和金黄色葡萄球菌基本无抑制作用.

4‐Hydroxy‐2 （1 H ）‐pyridone‐3‐carboxamide ,an ilicicolin H analogue ,was synthe‐sized with yield of 17% from trans‐4‐hydroxycinnamic acid through acetylation ,substitution , curtius rearrangement ,addition ,cyclization and so on .Its antifungal and antimicrobial activi‐ties were screened by filter paper diffusion method .Results indicated that the compound show potential antifungal activity against Candida albicans and weak activity against Yeast .The compound shows no inhibition effect on E .coli and Staphylococcus aureus .