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纳米级替考拉宁 ψ-糖基全氟碳簇合物。合成、抗菌活性和聚集研究。

Nano-sized clusters of a teicoplanin ψ-aglycon-fullerene conjugate. Synthesis, antibacterial activity and aggregation studies.

机构信息

Department of Pharmaceutical Chemistry, University of Debrecen, Medical and Health Science Center, Egyetem tér 1, H-4032 Debrecen, Hungary.

出版信息

Eur J Med Chem. 2012 Aug;54:943-8. doi: 10.1016/j.ejmech.2012.06.054. Epub 2012 Jul 4.

Abstract

Glycopeptide antibiotic derivative teicoplanin ψ-aglycone has been bound covalently to a fullerenopyrrolidine derivative using azide-alkyne 1,3-dipolar cycloaddition reaction. The aggregation of the antibiotic-fullerene conjugate in aqueous solution has been studied. The conjugate exhibited antibacterial activity against enterococci resistant to teicoplanin.

摘要

糖肽类抗生素衍生物替考拉宁 ψ-糖苷配基已通过叠氮-炔基 1,3-偶极环加成反应共价结合到富勒烯吡咯烷衍生物上。研究了该抗生素-富勒烯缀合物在水溶液中的聚集情况。该缀合物对耐替考拉宁的肠球菌表现出抗菌活性。

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