Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains |
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Authors: | Yan Ri-Bai Yuan Min Wu Yanfen You Xuefu Ye Xin-Shan |
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Institution: | a State Key Laboratory of Natural and Biomimetic Drugs, Peking University, School of Pharmaceutical Sciences, Peking University, Xue Yuan Road No. 38, Beijing 100191, China b Institute of Medicinal Biotechnology, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China |
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Abstract: | 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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Keywords: | Antibiotics Aminoglycoside Drug design Chemical modification Drug resistance |
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