Synthesis, structure and biological activity of pseudopeptidic macrolides based on an amino alcohol

A series of new pseudopeptidic macrolides 2a–f based on an amino alcohol were synthesized and evaluated for in vitro antibacterial and antifungal activities. The structure–activity relationships of these compounds were studied and the results showed that compounds 2a and 2d exhibited moderate antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli, whereas compound 2e showed potent antifungal activity against all the fungal species tested, showing a promising broad-spectrum antifungal activity. All the compounds have been studied in vitro for the hemolytic activity as a measure of their cytotoxicity, showing that these compounds have low lytic properties.

Synthesis, structure and biological activity of six new pseudopeptidic macrolides based on an amino alcohol are described.Figure optionsDownload as PowerPoint slide