THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
发明人:
BURKE, MARTIN D.,UNO, BRICE E.
申请号：
CA2981288
公开号：
CA2981288A1
申请日:
2015.05.15
申请国别(地区):
CA
年份:
2015
代理人:
摘要：
Disclosed is a derivative of amphotericin B (AmB), denoted C2epiAmB, with an improved therapeutic index over amphotericin B, pharmaceutical compositions comprising the AmB derivative, methods of making the AmB derivative and the pharmaceutical composition, and their use in methods of inhibiting growth of a yeast or fungus and treating a yeast or fungal infection. C2epiAmB is an epimer of the parent compound. Specifically, C2epiAmB differs from the parent compound at the C2 stereogenic center on mycosamine. This difference in structure results in (i) retained capacity to bind ergosterol and inhibit growth of yeast, (ii) greatly reduced capacity to bind cholesterol, and (iii) essentially no toxicity to human cells.
