Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains.

Yan RB; Yuan M; Wu YYou XYe XS

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Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains.

机译：Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains.

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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.

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来源
《Bioorganic and medicinal chemistry》 |2011年第1期|30-40|共11页
作者
Yan RB; Yuan M; Wu YYou XYe XS;
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State Key Laboratory of Natural and Biomimetic Drugs, Peking University, School of Pharmaceutical Sciences, Peking University, Xue Yuan Road No. 38, Beijing 100191, China.;

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正文语种英语
中图分类药学;
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Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains.

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