Synthesis and biological activity of tripeptidyl polyoxins as antifungal agents.
AUTOR(ES)
Naider, F
RESUMO
Three tripeptidyl polyoxins were synthesized and found to inhibit Candida albicans. Compared with the naturally occurring polyoxin D, the three synthetic polyoxins had little effect on chitin synthetase when assayed with a C. albicans membrane preparation. However, all the compounds inhibited growth, affected cell morphology in a manner similar to that of polyoxin D, and were hydrolyzed by cell extracts of C. albicans. Hydrolysis did not occur extracellularly, and at least one of the synthetic polyoxins, leucyl-norleucyl-uracil polyoxin C, inhibited peptide uptake, suggesting entrance into the cell via the peptide transport system. Thus, the intact tripeptidyl polyoxins are inactive prodrugs that are converted to active moieties by cellular enzymes.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=185943Documentos Relacionados
- Abasic oligodeoxyribonucleoside phosphorothioates: synthesis and evaluation as anti-HIV-1 agents.
- Biological monitoring of exposure to nerve agents.
- In vitro models for studying toxicity of antifungal agents.
- Pneumocystis carinii is resistant to imidazole antifungal agents.
- Reversal of the biological activity of Escherichia coli heat-stable enterotoxin by disulfide-reducing agents.