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学科主题: 药学
题名:
Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains
作者: Yan, Ri-Bai1; Yuan, Min2,3; Wu, Yanfen1; You, Xuefu2,3; Ye, Xin-Shan1
关键词: Antibiotics ; Aminoglycoside ; Drug design ; Chemical modification ; Drug resistance
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2011
DOI: 10.1016/j.bmc.2010.11.065
卷: 19, 期:1, 页:30-40
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: MOLECULAR RECOGNITION ; CRYSTAL-STRUCTURES ; TARGETING RNA ; RIBOSOMAL-RNA ; DERIVATIVES ; NEOMYCIN ; NEAMINE ; ENZYMES ; INHIBITION ; COMPLEXES
英文摘要:

Based on the structural information of biomacromolecule-aminoglycoside complexes, a series of kanamycin B analogues were rationally designed and synthesized. A convenient approach to the construction of kanamycin derivatives, in which the C4′-position on ring I of neamine moiety was modified, was developed. Most synthetic analogues exhibited good to excellent antibiotic activity against some typical drug-resistant bacteria. The disclosed results suggested that the C4′-position of aminoglycosides such as kanamycin may be an ideal site for modification to gain new modifying enzyme-resistant aminoglycoside antibiotics. (C) 2010 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 2009ZX09501-011
项目资助者: National Natural Science Foundation of China ; Ministry of Science and Technology of China
WOS记录号: WOS:000285724800003
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67467
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Union Med Coll, Inst Med Biotechnol, Beijing 100050, Peoples R China
3.Chinese Acad Med Sci, Beijing 100050, Peoples R China

Recommended Citation:
Yan, Ri-Bai,Yuan, Min,Wu, Yanfen,et al. Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(1):30-40.
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