肽脱甲酰基酶抑制剂的构效关系研究进展  

Progresses in the investigations of peptide deformylase inhibitors

作　　者：于慧杰[1] 周伟澄[1] 

机构地区：[1]上海医药工业研究院,上海200437

出　　处：《中国新药杂志》2005年第9期1102-1108,共7页Chinese Journal of New Drugs

基　　金：上海市科学技术委员会资助项目(04JC14068;04DZ05902)

摘　　要：肽脱甲酰基酶是细菌蛋白质合成过程中一种关键酶。肽脱甲酰基酶抑制剂通过作用于该酶,影响细菌正常的生长、代谢和繁殖,从而可能成为一类新型抗菌药物。许多拟肽类和非肽类化合物含有与金属离子结合的基团,表现出较高的肽脱甲酰基酶亲和力和较好的抗菌活性。综述该类药物的作用机制、结构修饰和构效关系。Peptide deformylase （PDF） is an essential enzyme involving in bacterial protein biosynthesis. The peptide deformylase inhibitors （PDFIs） block the growth, metabolism and muhiplication of bacteria, potentiating a novel type of antibacterial agent. Recent studies found that many non-peptide and peptidomimetic PDFIs with metal-binding groups have a high affinity to PDF and good antibacterial activity. In this review, the mechanism, structural modifications and structure-activity relationship of PDFIs are summarized.

关 键 词：肽脱甲酰基酶 肽脱甲酰基酶抑制剂 构效关系 抗菌药物 

分 类 号：R978.7[医药卫生—药品] R515[医药卫生—药学]