以糖修饰苯二氮类药物

目的以糖来修饰苯二氮类药物,寻找具有更高生物学活性的化合物,以期减少苯二氮类药物的毒副作用。方法以相关有机原料合成苯二氮类药物-糖化合物所需的原料,最终合成1-[3-(1-甲基-5-苯基-7-氯-1,3-二氢-2H-1,4-苯并二氮杂-2-酮)基]-D-吡喃葡萄糖苷。结果以地西泮为例,通过对地西泮进行结构修饰,在苯并二氮杂环的七元环的3位碳上连接葡萄糖,得到一个新的化合物。结论可以尝试对苯二氮类的其它药物进行结构修饰,在不同的位置连接上不同的糖,从中寻找具有更高生物活性的物质。

The saccharide modification of benzodiazepine drugs

OBJECTIVE Through the saccharide modification of Benzodiazepine drugs,expect to find some compounds which are more activated and to decrease adverse reaction.METHODS The paper describes the procedures for the saccharide derivatives synthesis and prepares the materials as follows:NIS;NBS;1-p-tolythio-2,3,4,6-tetra-O-acetyl-D-pyranglucoside;3-acetyloxy-7-chloro-1-methyl-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepine-2-one;3-hydroxy-7-chloro-1-methyl-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepine-2-one.Finally achieve...