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Structural modification of a specific antimicrobial lead against Helicobacter pylori discovered from traditional Chinese medicine and a structure-activity relationship study

文献类型：期刊论文

作者Zhang, Bang-Le1,2; Fan, Cheng-Qi1; Dong, Lei1; Wang, Fang-Dao1; Yue, Jian-Min1
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2010-11
卷号45期号:11页码:5258-5264
关键词Anti-Helicobacter pylori lead Structural modification SAR study
ISSN号0223-5234
DOI10.1016/j.ejmech.2010.08.045
文献子类Article
英文摘要Psoralen (1a) was found to be a specific and potent antimicrobial lead against Helicobacter pylori (H. pylori) from a traditional Chinese medicine (TCM) in the bioassay directed isolation. A series of structurally diverse analogues of la were thus designed and synthesized to improve the antimicrobial potency, some of which showed more potent activities than the lead compound (1a) against H. pylori. Among them, compound 25a is 16-fold stronger (MIC = 0.39 mu g/mL) than 1a (MIC = 6.25 mu g/mL), and is even potent than the positive control metronidazole (MIC = 0.50 mu g/mL). The in vitro antimicrobial activities against H. pylori of these structurally diverse analogues based on the scaffold of la have also led to an outline of structure-activity relationship. (C) 2010 Elsevier Masson SAS. All rights reserved.
WOS关键词XANTHOTOXIN DERIVATIVES ; GASTRIC-CANCER ; METRONIDAZOLE ; FUROCOUMARINS ; RESISTANCE ; INFECTION ; GROWTH
资助项目National Natural Science Foundation[30701044] ; Chinese Academy of Sciences[KSCX2-YW-R-117] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09301-001] ; Shanghai Municipal Scientific Foundation of the People's Republic of China[08JC1422300]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000283911300068
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/278738]  
专题天然药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Yue, Jian-Min
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
2.Fourth Mil Med Univ, Sch Pharm, Xian 710032, Shaanxi, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Bang-Le,Fan, Cheng-Qi,Dong, Lei,et al. Structural modification of a specific antimicrobial lead against Helicobacter pylori discovered from traditional Chinese medicine and a structure-activity relationship study[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2010,45(11):5258-5264.
APA Zhang, Bang-Le,Fan, Cheng-Qi,Dong, Lei,Wang, Fang-Dao,&Yue, Jian-Min.(2010).Structural modification of a specific antimicrobial lead against Helicobacter pylori discovered from traditional Chinese medicine and a structure-activity relationship study.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,45(11),5258-5264.
MLA Zhang, Bang-Le,et al."Structural modification of a specific antimicrobial lead against Helicobacter pylori discovered from traditional Chinese medicine and a structure-activity relationship study".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 45.11(2010):5258-5264.

入库方式： OAI收割

来源：上海药物研究所

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