amphotericin-b and eupolauridine

Eupolauridine, an indenonaphthyridine alkaloid, has been previously reported by us to exhibit antifungal activity. This study describes the synthesis of new alkyl and benzyl naphthyridinium/pyridinium analogs of eupolauridine as potential antifungal agents. A majority of the analogs exhibited antifungal activity against opportunistic pathogens such as Candida albicans and Cryptococcus neoformans. Several of them were also effective against bacteria (Staphylococcus aureus, MRS, Pseudomonas and Mycobacterium) and the malaria parasite (Plasmodium falciparum) to variable extents. A number of analogs were also cytotoxic to human cancer cell lines.

Topics: Amphotericin B; Animals; Anti-Bacterial Agents; Anti-Infective Agents; Antifungal Agents; Antimalarials; Antineoplastic Agents; Aspergillus fumigatus; Candida albicans; Cell Line, Tumor; Chlorocebus aethiops; Cryptococcus neoformans; DNA Topoisomerases, Type I; Humans; Indenes; Naphthyridines; Plasmodium falciparum; Structure-Activity Relationship; Topoisomerase I Inhibitors; Vero Cells