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[1]孙亦诚,徐斌,彭宇然,等.15-芳亚甲基脱水穿心莲内酯的合成与抗菌活性[J].南京工业大学学报(自然科学版),2016,38(04):79-87.[doi:10.3969/j.issn.1671-7627.2016.04.014]
 SUN Yicheng,XU Bin,PENG Yuran,et al.Synthesis and screening of 15-arylmethylene dehydroandrographolides as antibacterial agents[J].Journal of NANJING TECH UNIVERSITY(NATURAL SCIENCE EDITION),2016,38(04):79-87.[doi:10.3969/j.issn.1671-7627.2016.04.014]
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15-芳亚甲基脱水穿心莲内酯的合成与抗菌活性()
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《南京工业大学学报(自然科学版)》[ISSN:1671-7627/CN:32-1670/N]

卷:
38
期数:
2016年04期
页码:
79-87
栏目:
出版日期:
2016-07-10

文章信息/Info

Title:
Synthesis and screening of 15-arylmethylene dehydroandrographolides as antibacterial agents
文章编号:
1671-7627(2016)04-0079-09
作者:
孙亦诚1徐斌1彭宇然2姚忠3周国春1
1.南京工业大学 药学院,江苏 南京 211800; 2.南京工业大学 生物与制药工程学院,江苏 南京 211800; 3.南京工业大学 食品学院,江苏 南京 211800
Author(s):
SUN Yicheng1XU Bin1PENG Yuran2YAO Zhong3ZHOU Guochun1
1.College of Pharmaceutical Sciences,Nangjing Tech University,Nanjing 211800,China; 2.College of Biotechnology and Pharmaceutical Engineering,Nanjing Tech University,Nanjing 211800,China; 3.College of Food Sciences,Nanjing Tech University,Nanjing 211800,C
关键词:
脱水穿心莲内酯 衍生物 抗菌活性
Keywords:
dehydroandrographolide derivatives antibacterial activity
分类号:
R284.3
DOI:
10.3969/j.issn.1671-7627.2016.04.014
文献标志码:
A
摘要:
以脱水穿心莲内酯为原料与2个取代苯甲醛缩合得到2个15-芳亚甲基取代的脱水穿心莲内酯,进一步对其C-3,19位羟基衍生化,共得到14个衍生物,所有合成化合物均通过核磁共振仪(NMR)和高分辨质谱仪(HRMS)表征。在合成实验中,初步考察了C-3,19位乙酰化、C-3位羟基氧化和C-19位脱保护的方法。抗菌活性筛选实验研究发现,化合物G2对粪肠球菌的抑制能力优于脱水穿心莲内酯,有一定的研究价值。
Abstract:
Reaction of dehydroandrographolide and substituted benzaldehydes afforded two 15-arylmethylene dehydroandrographolides, derivatizing them generated 3,19-modified products of 15-arylmethylene dehydroandrographolides.14 Compounds of the derivatives were characterized by nuclear magnetic resonance(NMR)and high resolution mass spectra(HRMS).Reaction conditions for acetylation of C-3,19 hydroxyl groups,oxidation of the C-3 hydroxyl group and cleavage of the C-19 protecting group were investigated.Compound G2 had stronger activities to Enterococcus faecalis than that of dehydroandrographolide.

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备注/Memo

备注/Memo:
收稿日期:2015-03-06
基金项目:国家自然科学基金(30973621)
作者简介:孙亦诚(1989—),女,江苏金坛人,硕士,主要研究方向为化学合成药物; 姚忠(联系人),教授,E-mail: yaozhong@njtech.edu.cn.
引用本文:孙亦诚,徐斌,彭宇然,等.15-芳亚甲基脱水穿心莲内酯的合成与抗菌活性[J].南京工业大学学报(自然科学版),2016,38(4):79-87..
更新日期/Last Update: 2016-07-10