4-烃基脲取代Neu5Ac2en衍生物的合成筛选  

Synthesis and anti-influenza activity detection of 4-alkylcarbamido substituted Neu5Ac2en derivatives

作　　者：刘宗英[1] 李卓荣[1] 朱建华[1] 陶佩珍[1] 王淑琴[1] 邵华一[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《中国抗生素杂志》2006年第8期466-470,共5页Chinese Journal of Antibiotics

基　　金：国家自然科学基金资助项目(30371674)

摘　　要：目的合成若干4-烃基脲Neu5Ac2en衍生物并检测其抗病毒活性。方法以5-乙酰氨基-4β-氨基-7,8,9-三-O-乙酰基-2,3,4,5-四脱氧-D-甘油-D-半乳糖-壬-2-烯吡喃糖酸甲酯为起始原料,经过2步反应得到目标化合物,并对目标化合物进行抗病毒活性测定。结果目标化合物的结构均经过核磁共振、质谱确证。结论Neu5Ac2en的4-位被烃基脲替代后失去抗病毒活性。Objective To synthesize alkylcarbamido substituted Neu5Ac2en derivatives and detect antiinfluenza activity of them. Method The target compounds were prepared by a 2-step process using 5-aeetamido- 4-amino-7, 8, 9-tri-O-aeetyl-2, 3, 4, 5-tetradeoxy-D-galaeto-non-2-enonie acid methyl ester as starting material, their anti-influenza activity were evaluated. Result The structures of all the synthesized compounds were verified by ^1H-NMR and MS. Conclusion All the 4-alkylcarbamido substituted Neu5Ac2en derivatives have no anti-influenza activity under the testing concentration.

关 键 词：神经氨酸酶 流感病毒 Neu5Ac2en 脲基取代 

分 类 号：R978.7[医药卫生—药品]