黄酮C-7接枝氧肟酸的合成及尿素酶抑制活性研究  

Synthesis and Evaluation of Flavonoids Containing Hydroxamic Acid as Urease Inhibitors

作　　者：刘琦 师维康[1] 倪伟伟 龚思华 刘文润 徐宁 李腾飞 孙玉文 李玲霞 肖竹平[1] LIU Qi;Sill Wei-kang;NI Wei- wei;GONG Si-hua;LIU Wen-run;X U Ning;LI Teng-fei;SUN Yu-wen;LI Ling-xia;XIAO Zhu-ping(Hunan Engineering Laborato- ry for Analyse and Drugs Development of Ethnomedieine in Wuling Mountains, College of Chemistry and Chemical Engineering, Jishou University,Jishou 416000,China)

机构地区：[1]吉首大学化学化工学院武陵山地区民族药解析与创新湖南省工程实验室,湖南吉首416000

出　　处：《化学试剂》2017年第12期1263-1267,共5页Chemical Reagents

基　　金：国家自然科学基金资助项目(81273382);湖南省自然科学基金资助项目(2015JJ2116)

摘　　要：某些天然黄酮具有尿素酶抑制活性,为强化黄酮类化合物的尿素酶抑制作用,通过烷基化、肟化等步骤对7-羟基黄酮、白杨素、刺芒柄花素和大豆苷元进行了接枝衍生,分别用1HNMR、13CNMR、MS等方法对其进行结构表征,并研究其尿素酶抑制活性。活性测定表明,化合物4'-甲氧基异黄酮-7-基-O-乙酰氧肟酸和4'-羟基异黄酮-7-基-O-乙酰氧肟酸对尿素酶的抑制活性比阳性对照乙酰氧肟酸更好。其中,4'-羟基异黄酮-7-基-O-乙酰氧肟酸的IC50=(6.21±0.82)μmol/L。Some natural flavonoids were reported to possess moderate urease inhibitory activity.In order to improve the urease inhibition of flavonoids,7-O-side chain with hydroxamic acid of 7-hydroxyflavone,chrysin,formononetin and daidzein have been designed and synthesized by alkylation and oximation.The structures of these compounds were confirmed by1 HNMR,13 CNMR and MS,and their urease inhibitory activities were investigated. The activity assay showed that compounds 4＇-methoxyisoflavone-7-yloxyacetohydroxamic acid and 4＇-hydroxylisoflavone-7-yl-oxyacetohydroxamic acid displayed higher potency against urease than that of positive control acetohydroxamic acid. The most active 4＇-hydroxylisoflavone-7-yl-oxyacetohydroxamic acid showed IC50 of（6. 21±0. 82） μmol/L.

关 键 词：黄酮 结构改造 氧肟酸 幽门螺旋杆菌 尿素酶抑制剂 

分 类 号：R914.5[医药卫生—药物化学]