Glycosylation of fluoroquinolones through direct and oxygenated polymethylene linkages as a sugar-mediated active transport system for antimicrobials

…, BT Vu, M Kiankarimi, E Spyrou, J Kaunitz

文献索引：Jung, Michael E.; Yang, Eric C.; Vu, Binh T.; Kiankarimi, Mehrak; Spyrou, Emmanouil; Kaunitz, Jon Journal of Medicinal Chemistry, 1999 , vol. 42, # 19 p. 3899 - 3909

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被引用次数: 32

摘要

We report herein the synthesis and biological testing of several glycosylated derivatives of some fluoroquinolone antibiotics. In particular, we have prepared several glycosylated derivatives of ciprofloxacin (2) in which the carbohydrate units are linked to the free secondary amine of the piperazine unit by:(a) no linker (eg, a glycosylamine),(b) a β- oxyethyl linker, and (c) a γ-oxypropyl linker. Both glucose and galactose were used as ...