欢迎您！东篱公司
退出
-
申报数据库
-
立项数据库
-
成果数据库
-
项目获奖数据库
中文摘要：
目的设计合成格列本脲衍生物并进行降血糖活性研究。方法以5-氯-2-甲氧基苯甲酸为原料,经甲基化、胺解、氯磺化、氮化、缩合反应得到格列本脲二氟衍生物。通过链脲佐菌素（streptozotocin,STZ）配合高脂饲料诱发大鼠Ⅱ型糖尿病模型,评价其降血糖作用。结果经过5步反应合成目标化合物格列本脲二氟衍生物,总收率为28.1%,目标化合物和中间体的结构经1H-NMR和MS确证。活性实验显示格列本脲二氟衍生物具有明显降糖作用。结论在格列本脲的环己烷对位上用2个氟原子取代有利于增加其降血糖活性。
英文摘要：
Objective To research on design,synthesis and hypoglycemia activity of glibenclamide derivative. Methods The synthesis of 4＇,4＇-difluoroglibenclamide derivative had been accomplished from 5-chloro-2-methoxybenzoic acid,through five steps in 28. 1% overall yield（ based on 5-chloro-2-methoxybenzoic acid）,including methylation,aminolysis,chlorosulfonation,nitrification and condensation reactions. Its hypolycemic effect w as observed in type 2 diabetic rat model induced by high lipid food plus STZ. Results The target structure w as identified by ESI-M S and1H-NM R,and the result of hypoglycemic effect show ed that the difluoroglibenclamide had pow erful hypoglycemic activity. Conclusions It＇s a good strategy to increase hypoglycemic activity by introducing tw o fluorine atoms into glibenclamide.
同期刊论文项目
同项目期刊论文
Synthesis and biological evaluation of substituted 1,2,3-benzotriazines and pyrido[3,2-d]-1,2,3-tria
Stereochemical Investigation of a Novel Biological Active Substance from the Secondary Metabolites o
Insight into the Development of Dissolution Media for BCS Class II Drugs: A Review from Quality Cont
Design and synthesis of novel 2-(4-(2-(dimethylamino)ethyl)-4H-1,2,4-triazol-3-yl)pyridines as poten
A study of Semen Strychni-induced renal injury and herb–herb interaction of Radix Glycyrrhizae extra
Comparative pharmacokinetics of cyclophosphamide administration alone and combination with vitamin B
Comparative pharmacokinetics study of a kaurane diterpenoid after oral administration of monomer and
Simultaneous determination of seven residual pharmaceuticals in wastewater by solid-phase extraction
Study on molecular structure, spectroscopic investigation(IR, Raman and NMR), vibrational assignment
Determination of larotaxel and its metabolites in rat plasma by liquid chromatography-tandem mass sp
Simultaneous determination of eight active components in chloroform extracts from raw and vinegar-pr
Rapid extraction and analysis method for the simulaneous determination of 21 bioflavonoids in Sieges
The Crystal Structure of 3-(4-Methoxyphenyl)-2-(4-methylbenzoyl)-6,7-dihydro-5H-furo[3,2-g] chromene
Enantioseletive skin permeation of ibuprofen enantiomers: mechanistic insights from ATR-FTIR and CLS
Density functional theory (DFT) and natural bond orbital (NBO) study of vibrational spectra and intr
Identification and Optimization of New Dual Inhibitors of B-Raf and Epidermal Growth Factor Receptor
Simultaneous determination of reserpine, yohimbine and ajmalicine in the extract of Rauvolfia rootst
Simultaneous determination of Rutin, Luteolin, Quercetin, and Betulinic acid in the extract of dispo
A sample, one-pot synthesis of trans-substituted spiro[5,5] undecane-1,5,9-triones with aromatic ald
期刊信息
位置：