Benanomicin A is produced by the strain of Actinomadura sp. MH193-16F4. A and B have anti-candida, Cryptococcus neoforme, Saccharomyces cerevisiae and other fungal activities, while A has stronger activity. Xylose benamycin A and B showed similar or slightly stronger activity against candida, yeast and Cryptococcus, but decreased activity against aspergillus. The antifungal activity of 2-demethylbenamycin was similar to that of xylose Benamycin A. The synthesized 7-methoxybenamycin had little antifungal activity, but showed inhibitory activity of glucosinolase (EC 3.2.1.20) with IC50 of 60μg/mL.