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两性霉素 B(AmB)是多烯大环内酯中非芳香七烯类的抗生素,是治疗各种深部真菌感染的首选药物。由于它有一系列毒副反应(如损伤肾功能等)和水不溶性,因此临床的应用受了限制。而究其根本则是因为 AmB与动物和真菌细胞的靶、膜的胆甾醇和麦角甾醇的相互作用缺乏选择性。长期以来,人们赏试合成低毒性、水溶性的 AmB 衍生物,包括一系列的酯、酰胺、N-酰基、N-烷基
Amphotericin B (AmB) is a non-aromatic heptapene antibiotic in polyene macrolide and is the drug of choice for the treatment of various deep fungal infections. Because of its series of toxic side effects (such as damage to renal function, etc.) and water insoluble, the clinical application is limited. The fundamental reason is because AmB and animal and fungal cells target, the lack of selectivity of membrane cholesterol and ergosterol interaction. For a long time, people try synthesis of low toxicity, water-soluble AmB derivatives, including a series of esters, amides, N-acyl, N-alkyl