应用化学2012，Vol.29Issue(8)：873-877,5.DOI:10.3724/SP.J.1095.2012.00371
甘草次酸3位氨基酸衍生物的合成及其抑菌活性
Synthesis and Activity of 3-Amino Acid Derivatives of Glycyrrhetinic Acid
王军 1胡小丽 2文伟河 2杨雷雷 2朱玉亮2
作者信息
- 1. 江苏警官学院公安科技系 南京210012
- 2. 南京工业大学生物与制药工程学院 南京210009
- 折叠
摘要
Abstract
In order to obtain more effective glycyrrhetinic derivatives, 3-amino acid derivatives were synthesized from glycyrrhetinic acid via deoxidation of the 11-carbonyl group, ethyl esterification of the 30-carboxylic group and esterification of 3-hydroxyl group using Fmoc-protected amino acids, which include methionine, threonine, valine and phenylalanine, by dicyclohexylcarbodiimide(DCC)/dirnethylaminopyridine (DMAP) coupling method in tetrahydrofuran. The final products were obtained by removing Fmoc using F(CH2C12):F((C2H5)2NH) =1:1 solvent mixture with 80% -87% yields and characterized by 'H NMR and MS. Preliminary pharmacological research showed that compounds 5a - 5d could protect the growth of E col. , Bacillus Subtilis and Yeast against high level of N,N-dimethylformamide.关键词
甘草次酸/Fmoc保护氨基酸/还原/酯化/脱保护Key words
glycyrrhetinic,Fmoc protected amino acids,deoxidation,esterification,deprotect分类
化学化工引用本文复制引用
王军,胡小丽,文伟河,杨雷雷,朱玉亮..甘草次酸3位氨基酸衍生物的合成及其抑菌活性[J].应用化学,2012,29(8):873-877,5.
