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去氢表雄酮结构修饰物的合成及其抗菌活性评价
引用本文:陶洪文,王江伟,彭可睿,李筱芳,于贤勇,陈建,易平贵.去氢表雄酮结构修饰物的合成及其抗菌活性评价[J].湖南科技大学学报(自然科学版),2015,30(1):104-109.
作者姓名:陶洪文  王江伟  彭可睿  李筱芳  于贤勇  陈建  易平贵
作者单位:湖南科技大学化学化工学院,理论化学与分子模拟省部共建教育部重点实验室,分子构效关系湖南省普通高等学校重点实验室;中国药科大学药学院
基金项目:国家自然科学基金资助项目(21172066);湖南科技大学理论化学与分子模拟省部共建教育部重点实验室开放基金(E21203)
摘    要:以去氢表雄酮为原料,通过环氧化、环氧开环、内酯化和酯化等化学反应,合成了9个结构修饰物,产物经核磁共振、质谱和红外光谱等进行表征,并进一步进行了初步的抗菌活性测试,结果显示2个化合物对金黄色葡萄球菌具有中等抑制活性,6个化合物对枯草芽孢杆菌具有中等抑制活性,4个化合物对白色念珠菌具有弱抑制活性.

关 键 词:去氢表雄酮  结构修饰  合成  抗菌

Synthesis and antimicrobial activity evaluation of modified compounds from dehydroepiandrosterone
Tao Hongwen,Wang Jiangwei,Peng Kerui,Li Xiaofang,Yu Xianyong,Chen Jian,Yi Pinggui.Synthesis and antimicrobial activity evaluation of modified compounds from dehydroepiandrosterone[J].Journal of Hunan University of Science & Technology(Natural Science Editon),2015,30(1):104-109.
Authors:Tao Hongwen  Wang Jiangwei  Peng Kerui  Li Xiaofang  Yu Xianyong  Chen Jian  Yi Pinggui
Institution:Tao Hongwen;Wang Jiangwei;Peng Kerui;Li Xiaofang;Yu Xianyong;Chen Jian;Yi Pinggui;Key Laboratory of Theoretical Chemistry and Molecular Simulation of Ministry of Education,Hunan Province College Key Laboratory of QSAR / QSPR,School of Chemistry and Chemical Engineering,Hunan University of Science and Technology;School of Pharmacy,China Pharmaceutical University;
Abstract:Nine modified compounds were synthesized by epoxidation, epoxide ring opening, lactonization and esterification reactions using dehydroepiandrosterone(DHEA) as starting material. The products were identified by NMR, MS and IR analysis. Furtherly, the preliminary antimicrobial activities of these compounds were evaluated. Two compounds exhibited moderate inhibition against Staphylococcus aureus. Six compounds showed moderate inhibition against Bacillus subtilis. Four compounds exhibited weak inhibition against Candida albicans.Keywords: dehydroepiandrosterone;chemical modification; synthesis;antimicrobial
Keywords:dehydroepiandrosterone  chemical modification  synthesis  antimicrobial
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