作　　者： (马献力）; (黄琳）; (苏燕）; (龚红菲）; (庞富华）; (林家迅）; (李芳耀）;

机构地区： 桂林医学院药学院,广西桂林541004

出　　处： 《精细化工》 2017年第9期1023-1029,共7页

摘　　要： 以丹皮酚(2-羟基-4-甲氧基苯乙酮)(Ⅰ)为原料,与水合肼反应得到中间体丹皮酚腙(Ⅱ),然后Ⅱ分别与各种取代苯甲醛反应合成了9个N-苄叉丹皮酚腙(Ⅲa~Ⅲi),产率为50.5%~91.9%。利用FTIR、1HNMR、13CNMR、LC-MS对目标化合物的结构进行了表征。初步探索了Ⅱ和Ⅲ的合成条件、测定了Ⅲa~Ⅲi的抗菌活性。结果表明:化合物N-(4-氟苄叉基)丹皮酚腙(Ⅲc)对金黄色葡萄球菌的最低抑菌浓度(MIC)为2 mg/L,化合物N-(2-氟苄叉基)丹皮酚腙(Ⅲb)对大肠杆菌的MIC为8 mg/L,与阳性对照药利福平抗菌效果相当。 Intermediate Ⅱ was prepared from 2-hydroxy-4-methoxyphenylethanone（ Ⅰ） with hydrazine hydrate. Subsequently,nine novel N-benzylidene paeonol hydrazones（ Ⅲ a ~ Ⅲ i）） were synthesized via condensation reactions between intermediate Ⅱ and various benzaldehydes,respectively. Their yields were from 50. 5% to 91. 9%. These targeted products were confirmed by FTIR,1HNMR,13 CNMR and LC-MS techniques. Meanwhile,the synthetic conditions were initially explored. The preliminary bioassay showed that minimal inhibitory concentration（ MIC） of N-（ 4-fluorobenzylidene）paeonol hydrazone（ Ⅲc） against S. aureus A209 was 2 mg/L. While N-（ 2-fluorobenzylidene） paeonol hydrazone（ Ⅲb） possessed similar activity against E. coli ATCC25922 in comparison with rifampin as positive control drug,and the MIC was 8 mg/L.

关 键 词： 丹皮酚 丹皮酚腙 苄叉 抗菌活性 医药与日化原料