Paquet Valérie, Carreira Erick M
Laboratorium für Organische Chemie, ETH Hönggerberg, CH-8093 Zürich, Switzerland.
Org Lett. 2006 Apr 27;8(9):1807-9. doi: 10.1021/ol060353o.
[reaction: see text] New derivatives of Amphotericin B (AmB) were synthesized through a double reductive alkylation of the mycosamine. These derivatives of AmB displayed superior antifungal activity against Saccharomyces cerevisiae wild-type strain and especially in the case of an AmB-resistant Candida albicans strain. Moreover, these compounds are potential drug candidates because of significantly reduced hemotoxicity compared to AmB. Furthermore, the same mycosamine modification can be applied to other polyene macrolides such as Nystatin and Pimaricin to improve their antifungal activity.
[反应：见正文] 通过霉菌胺的双还原烷基化反应合成了两性霉素B（AmB）的新衍生物。这些AmB衍生物对酿酒酵母野生型菌株显示出优异的抗真菌活性，特别是对耐AmB的白色念珠菌菌株。此外，由于与AmB相比血液毒性显著降低，这些化合物是潜在的候选药物。此外，相同的霉菌胺修饰可应用于其他多烯大环内酯类药物，如制霉菌素和匹马霉素，以提高它们的抗真菌活性。
