期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 1, 页码 30-40出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.11.065
关键词
Antibiotics; Aminoglycoside; Drug design; Chemical modification; Drug resistance
资金
- National Natural Science Foundation of China
- Ministry of Science and Technology of China [2009ZX09501-011]
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.
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