Wang Jinhua, Li Jie, Chen Hsiao-Nung, Chang Huiwen, Tanifum Christabel Tomla, Liu Hsiu-Hsiang, Czyryca Przemyslaw G, Chang Cheng-Wei Tom
Department of Chemistry and Biochemistry, Utah State University, 0300 Old Main Hill, Logan, Utah 84322-0300, USA.
J Med Chem. 2005 Oct 6;48(20):6271-85. doi: 10.1021/jm050368c.
In an effort to optimize the antibacterial activity of kanamycin class aminoglycoside antibiotics, we have accomplished the synthesis and antibacterial assay of new kanamycin B analogues. A rationale-based glycodiversification strategy was employed. The activity of the lead is comparable to that of commercially available kanamycin. These new members, however, were found to be inactive against aminoglycoside resistant bacteria. Molecular modeling was used to provide the explanation. Thus, a new strategy for structural modifications of kanamycin class aminoglycosides is suggested.
为了优化卡那霉素类氨基糖苷类抗生素的抗菌活性，我们完成了新型卡那霉素B类似物的合成及抗菌测定。采用了基于原理的糖多样化策略。先导化合物的活性与市售卡那霉素相当。然而，这些新成员对氨基糖苷类耐药菌无活性。利用分子建模对此进行了解释。因此，提出了一种卡那霉素类氨基糖苷类结构修饰的新策略。
