[EN] MEMBRANE-TARGETING AMINOGLYCOSIDE-BASED CATIONIC AMPHIPHILES AND THERAPEUTIC USES<br/>[FR] AMPHIPHILES CATIONIQUES À BASE D'AMINOGLYCOSIDE, CIBLANT LES MEMBRANES, ET UTILISATIONS THÉRAPEUTIQUES
申请人:UNIV RAMOT
公开号:WO2014013495A1
公开(公告)日:2014-01-23
The present invention relates to amphiphilic aminoglycoside (AG) derivatives, especially derivatives of tobramycin, kanamycin A and paromomycin comprising hydrophobic side chains linked to the AG moiety by various linkers. These novel derivatives are useful as broad spectrum antibacterial agents targeting bacterial cell membranes, while having minimal toxicity due to non-selective targeting of eukaryotic cell membranes. The present invention further relates to methods for preparing the novel derivatives, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as membrane-targeting antibacterial agents for treating bacterial infections, and for inhibiting bio film growth.
本发明涉及两性的氨基糖苷(AG)衍生物,特别是托布拉霉素、卡那霉素A和帕罗莫霉素的衍生物,这些衍生物包括通过各种连接剂连接到AG基团的疏水侧链。这些新颖的衍生物可用作靶向细菌细胞膜的广谱抗菌剂,同时由于对真核细胞膜的非选择性靶向作用,具有最小毒性。本发明还涉及制备这些新颖衍生物的方法、包括这些化合物的药物组合物、以及使用这些化合物和组合物的方法,特别是作为靶向细菌细胞膜的抗菌剂,用于治疗细菌感染和抑制生物膜生长。