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肽脱甲酰化酶抑制剂的合成及其抑菌活性
引用本文:孟丽娟,汤立达,贾炯,徐为人,张大同,张士俊,王平保,冯勇,任戎,王建武.肽脱甲酰化酶抑制剂的合成及其抑菌活性[J].合成化学,2006,14(3):229-233,243.
作者姓名:孟丽娟  汤立达  贾炯  徐为人  张大同  张士俊  王平保  冯勇  任戎  王建武
作者单位:1. 山东大学,化学与化工学院,山东,济南,250100
2. 山东大学,化学与化工学院,山东,济南,250100;天津药物研究院,天津,300193
3. 天津药物研究院,天津,300193
基金项目:国家重点基础研究发展计划(973计划)
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。

关 键 词:肽脱甲酰化酶  抑制剂  合成  抑菌活性
文章编号:1005-1511(2006)03-0229-05
收稿时间:2005-12-26
修稿时间:2005-12-26

Synthesis of Peptide Deformylase Inhibitor and Their Bacteriostasis Activity
MENG Li-juan,TANG Li-da,JIA Jiong,XU Wei-ren,ZHANG Da-tong,ZHANG Shi-jun,WANG Ping-bao,FENG Yong,REN Rong,WANG Jian-wu.Synthesis of Peptide Deformylase Inhibitor and Their Bacteriostasis Activity[J].Chinese Journal of Synthetic Chemistry,2006,14(3):229-233,243.
Authors:MENG Li-juan  TANG Li-da  JIA Jiong  XU Wei-ren  ZHANG Da-tong  ZHANG Shi-jun  WANG Ping-bao  FENG Yong  REN Rong  WANG Jian-wu
Institution:1, School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China; 2. Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
Abstract: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.
Keywords:peptide deformylase  inhibitor  synthesis  bacteriostasis activity
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