Peptide dendrimers as antifungal agents and carriers for potential antifungal agent-N-3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic acid-synthesis and antimicrobial activity

摘要

A series of peptide dendrimers and their conjugates with antimicrobial agent FMDP (N-3-(4-methoxyfumaroyl)-(S)-2,3-diamino-propanoic acid) were synthesized. The obtained compounds were tested for the antibacterial and antifungal activity. All novel dendrimers displayed much better activity against the tested strains than FMDP itself. Moreover, their conjugates with FMDP also exhibited antimicrobial activity. The most promising molecules were tested against a broad selection of fungal strains. The analysis of their antifungal properties indicates that the examined molecules are efficient growth inhibitors of fluconazole-resistant hospital-acquired strains. Moreover, an application of amphiphilic branched peptides such as FMDP carriers suggests that transport mechanism involves more likely the cell membrane perturbation than the mediation of the specific transport proteins. The activity of obtained compounds strongly depends on the specific structure of the molecule.