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| 新型肽脱甲酰基酶(PDF)抑制剂的研究(Ⅰ) --含异噁唑的丁二酰异羟肟酸衍生物的设计与合成 | |
| 引用本文： | 汤立达,贾炯,徐为人,张大同,张士俊,郑晓平,王平保,冯勇,郑洪艳,李炎,刘登科,孟丽娟,任戎,王建武.新型肽脱甲酰基酶(PDF)抑制剂的研究(Ⅰ) --含异噁唑的丁二酰异羟肟酸衍生物的设计与合成[J].中国新药杂志,2006,15(10):797-801. |
| 作者姓名： | 汤立达 贾炯 徐为人 张大同 张士俊 郑晓平 王平保 冯勇 郑洪艳 李炎 刘登科 孟丽娟 任戎 王建武 |
| 作者单位： | 1. 山东大学化学与化工学院,济南,250100;天津药物研究院,天津,300193 2. 山东大学化学与化工学院,济南,250100 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： | 目的：发现新的肽脱甲酰基酶（PDF）抑制剂先导化合物.方法：在异噁唑环杂原子作为电子对供体替代羰基氧原子与受体形成氢键的新思路指导下,设计并合成了一系列新型含异噁唑的β-戊基-丁二酰异羟肟酸衍生物,其结构经核磁共振（NMR）、质谱（MS）等证明,并对部分该类化合物进行了体外抑菌实验.结果：体外抑菌实验表明,该类化合物具有一定的抗菌活性.结论：以异噁唑环杂原子作为电子对供体替代肽分子中的羰基氧原子与受体形成氢键的设想是成立的,为进一步优化本类化合物结构,乃至对类肽新药的设计具有重要意义. |
| 关 键 词： | 异唑 丁二酰异羟肟酸衍生物 肽脱甲酰基酶抑制剂 抗菌活性 |
| 文章编号： | 1003-3734（2006）10-0797-05 |
| 修稿时间： | 2005-12-27 |
A novel bacterial peptide deformylase inhibitor: synthesis of succinate hydroxamate analogues containing isoxazole substitute |
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| TANG Li-da,JIA Jiong,XU Wei-ren,ZHANG Da-tong,ZHANG Shi-jun,ZHENG Xiao-ping,WANG Ping-bao,FENG Yong,ZHENG Hong-yan,LI Yan,LIU Deng-ke,MENG Li-juan,REN Rong,WANG Jian-wu.A novel bacterial peptide deformylase inhibitor: synthesis of succinate hydroxamate analogues containing isoxazole substitute[J].Chinese Journal of New Drugs,2006,15(10):797-801. | |
| Authors: | TANG Li-da JIA Jiong XU Wei-ren ZHANG Da-tong ZHANG Shi-jun ZHENG Xiao-ping WANG Ping-bao FENG Yong ZHENG Hong-yan LI Yan LIU Deng-ke MENG Li-juan REN Rong WANG Jian-wu |
| Institution: | 1 School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China; 2 Tianfin Institute of Pharmaceutical Research, Tianfin 300193, China |
| Abstract: | Objective:To develop lead compounds classified as a nonpeptide bacterial peptide deformylase (PDF) inhibitor.Methods:Based on a rational that a heteroatom in isoxazole ring may be used as electron donor to form a hydrogen bond with receptors instead of oxygen atom in a carboxyl group of PDF,a series of 2-n-pentyl succinate hydroxamate derivatives containing isoxazole substitutes were newly synthesized.The structures of such new derivatives were confirmed by NMR and MS.An anti-bac- terial assay in vitro for the new derivatives was conducted.Results:The new derivatives showed antibac- terial activities.Conclusion:Isoxazole ring could be used as the substitute of amide to offer electron pairs for the formation of hydrogen bond with receptors. |
| Keywords: | isoxazole-contained 2-n-pentyl succinate hydroxamate peptide deformylase inhibitor antibacterial activity |
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