Template Synthesis of CPP32 Inhibitors by Ugi Four-Component Condensation Reaction  

经Ugi四组分缩合反应合成CPP32抑制剂模板(英文)

作　　者：张欣[1] 邹晓民[1] 傅翌秋[1] 杨晓鸣[1] 牟科[1] 徐萍[1] 

机构地区：[1]北京大学药学院药物化学系,北京100083

出　　处：《Journal of Chinese Pharmaceutical Sciences》2004年第4期238-241,共4页中国药学（英文版）

基　　金：NationalNaturalScienceFoundationofChina(2 0 2 72 0 0 4) .

摘　　要：To find a reasonable way to prepare the designed CPP32 inhibitors. Method Ugifour-component condensation reaction was used to synthesize peptide mimic CPP32 inhibitors; ResultsA key isocyanide component (aspartate-derived isocyanide 3) and one of the designed CPP32inhibitors 4 (as a template) were synthesized; Conclusion The CPP32 inhibitor 4 was synthesized bythe newly developed procedure, which is an Ugi four-component condensation reaction based onaspartate-derived isocyanide 3. This method can be used to build up the CPP32 inhibitor library.目的　找到合适途径来制备所设计的CPP32抑制剂。方法　Ugi四组分缩合反应用于合成拟肽类CPP32抑制剂。结果　合成了关键异腈组分 (天冬氨酸衍生异腈 3)和CPP32抑制剂模板分子 4。结论　以基于天冬氨酸衍生异腈 3的Ugi四组分缩合反应 ,合成了CPP32抑制剂 4。此新建的方法可用于构建CPP32拟肽类抑制剂化学库。

关 键 词：CPP32 Ugi-4CR ISOCYANIDE 

分 类 号：R914.4[医药卫生—药物化学]