Antifungal/Echinocandin B Derivatives: Novel Fungal Cell Wall Glucan Synthetase Inhibitors

Summary

Novelty: New antibiotic substances produced by the cultivation of Zalerion arboricola are described. The compounds are cyclic lipopeptides and are claimed as potential agents for Pneumocystis carinii, Candida albicans and Candida parapsilosis infections.

Biology: The tested compound has an IC₅₀ = 0.5μg/ml against Candida albicans (MY 1055), 16-128 μg/ml against Candida parapsilosis (MY 1009). One compound gave 66% reduction of Pneumocystis carinii cysts in C3H/He mice at 2 mg/kg (given for seven days).

Chemistry: 1-[N²-(10,12-dimethyl-1-oxotetradecyl)ornithine]-4-[4-hydroxyphenyl)-2-aminobutanoic acid]-5-(3-hydroxyglutamine) echinocandin B is one exemplified compound.