肽脱甲酰化酶抑制剂的合成及其抑菌活性  

Synthesis of Peptide Deformylase Inhibitor and Their Bacteriostasis Activity

作　　者：孟丽娟[1] 汤立达[1] 贾炯[1] 徐为人[2] 张大同[1] 张士俊[2] 王平保[2] 冯勇[1] 任戎[2] 王建武[1] 

机构地区：[1]山东大学化学与化工学院,山东济南250100 [2]天津药物研究院,天津300193

出　　处：《合成化学》2006年第3期229-233,243,共6页Chinese Journal of Synthetic Chemistry

基　　金：国家重大基础研究前期研究专项资助项目(2003CCA027)

摘　　要：通过对肽脱甲酰化酶抑制剂构效关系的研究,以放线酰胺素为先导化合物,设计并合成了一系列异噁唑类化合物。其结构经1H NMR,IR,MS和元素分析表征。生物活性实验表明,该类化合物对标准肺炎克雷白球菌有显著的抑菌活性。According to the structure-activity relationship of peptide deformylase inhibitors, a series of hydroxamic acid derivatives containing isoxazole were designed and synthesized based on the structure of actinonin. The structures of compounds were characterized by ^1H NMR, IR, MS and elemental analysis. The preliminary biological test showed that some compounds exhibited bacteriostasis activities.

关 键 词：肽脱甲酰化酶 抑制剂 合成 抑菌活性 

分 类 号：O629.8[理学—有机化学]