中文摘要：

泛素．蛋白酶体途径是细胞内降解蛋白质的一种主要方式，由20S蛋白酶体来完成蛋白质的降解。本文在已经报道的肽类抑制剂的基础上，设计合成了一类三肽四氮唑化合物，通过’HNMR、MS以及元素分析对化合物结构进行了表征。活性评价结果表明，有3个目标化合物（6b、6d和6h）具有较好的抑制20S蛋白酶体类胰凝乳蛋白酶的活性。分子对接研究显示，这类新型C端基肽类化合物能通过与活性位点非共价相互作用而与蛋白酶体结合。

英文摘要：

Ubiquitin-proteasome pathway （UPP） is one of the ways utilized for selective degradation of many proteins in cells, and the 20S proteasome takes the functional machinery where hydrolysis of targeted proteins takes place. Based on existing peptide inhibitors, a series of novel tripeptidic tetrazoles have been designed, synthesized, and the structures have been confirmed with IH NMR, MS and elemental analysis. Among them, three compounds （6b, 6d and 6b） showed inhibitory activities ofChT-L of20S proteasome.