肽脱甲酰基酶抑制剂LBM-415的研究进展  

The advance of the peptide deformylase inhibitor LBM-415

作　　者：周娜[1] 李祎亮[2] 徐为人[2] 汤立达[2] 

机构地区：[1]天津医科大学,天津300070 [2]天津药物研究院,天津300193

出　　处：《中国新药杂志》2007年第14期1137-1141,共5页Chinese Journal of New Drugs

摘　　要：肽脱甲酰基酶(PDF)作为细菌蛋白质合成过程中的关键酶之一,是一种较理想的抗微生物药物作用靶点。随着PDF晶体结构和作用机制的阐明,PDF抑制剂的研究已经成为近年来抗菌领域研究开发的热点。LBM-415(原名NVP-PDF-713)是一种已经进入临床研究的PDF抑制剂,研究表明其对多种病原菌均有显著的抑制活性。现就其合成方法、药理作用、药动学等方面的研究进行综述。As a key enzyme in the synthesis of bacteria protein, peptide deformylase（PDF） is an ideal target of antimicrobial drugs. With the interpretation of its crystal structure and mechanism of action, research on PDF inhibitors has become a new focus in the field of antibiosis. LBM-415 is one of the peptide deformylase inhibitors which has entered clinical evolution, research indicates it has notable activity to many pathogenic bacteria. Its synthesis, pharmacological actions and pharmacokinetics are reviewed in this paper.

关 键 词：肽脱甲酰基酶 肽脱甲酰基酶抑制剂 LBM-415 蛋白质合成 

分 类 号：R978.1[医药卫生—药品]