化学研究
化學研究
화학연구
CHEMICAL RESEARCHES
2015年
2期
153-157
,共5页
4-羟基-2(1 H )-吡啶酮-3-甲酰胺%冬青生菌素类似物%合成%抗真菌
4-羥基-2(1 H )-吡啶酮-3-甲酰胺%鼕青生菌素類似物%閤成%抗真菌
4-간기-2(1 H )-필정동-3-갑선알%동청생균소유사물%합성%항진균
4-hydroxy-2 (1 H )-pyridone-3-carboxamide%ilicicolin H analogue%synthesis%anti-fungal activity
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。
以反式‐4‐羥基肉桂痠為起始原料,經乙酰化、酰基疊氮、curtius重排、加成和環閤等6步反應閤成瞭4‐羥基‐2(1 H )‐吡啶酮‐3‐甲酰胺類鼕青生菌素類似物,總收率17%。隨後用濾紙片擴散法對該化閤物的抑菌性能進行瞭初步研究。實驗錶明,該化閤物對于白色唸珠菌具有較好的抑製作用,對于酵母菌抑製作用較弱,對大腸桿菌和金黃色葡萄毬菌基本無抑製作用。
이반식‐4‐간기육계산위기시원료,경을선화、선기첩담、curtius중배、가성화배합등6보반응합성료4‐간기‐2(1 H )‐필정동‐3‐갑선알류동청생균소유사물,총수솔17%。수후용려지편확산법대해화합물적억균성능진행료초보연구。실험표명,해화합물대우백색념주균구유교호적억제작용,대우효모균억제작용교약,대대장간균화금황색포도구균기본무억제작용。
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 .