Synthesis and structure-activity relationships of amides of amphotericin B.

Abstract

A series of aliphatic amides of amphotericin B have been synthesized. The structure of the derivatives which were obtained has been established by mass spectrometry. Their biological properties: inhibition of growth of Saccharomyces cerevisiae and hemolytic activity have been determined. The quantitative relationships between the activity of amides of amphotericin B against S. cerevisiae and their lipophilicity can be expressed by a parabolic function, whereas that between hemolytic activity and lipophilicity--by polynominal expression of fourth degree.