申请人:Chu Daniel
公开号:US20060276623A1
公开(公告)日:2006-12-07
Semi-synthetic glycopeptides having antibacterial activity are based on modifications of the eremomycin, A82846B, vancomycin, teicoplanin, and A-40,926 scaffolds, in particular, acylation of the sugar moieties on these scaffolds with certain acyl groups; and/or conversion of an acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides; or having a combination of an alkylation modification of the amino substituent on the amino-substituted sugar moiety on these scaffolds with certain alkyl groups or acylation modification of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain alkyl groups, and conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
具有抗菌活性的半合成糖肽基于对eremomycin、A82846B、vancomycin、teicoplanin和A-40,926骨架进行修改,特别是用特定酰基对这些骨架上的糖基进行酰化;和/或将这些骨架上的大环环上的酸基转化为特定的取代酰胺;或者将这些骨架上氨基取代糖基上的氨基取代物进行烷基化修改,使用特定烷基基团或将这些骨架上氨基取代糖基上的氨基取代物进行酰基化修改,以及将这些骨架上的大环环上的酸基转化为特定的取代酰胺的组合。还提供了合成这些化合物的方法,包含这些化合物的药物组合物,以及用于治疗和/或预防疾病,特别是细菌感染的方法。