Several 13-alkyl substituted analogs of berberine and palmatine were found to be highly active against two types of Staphylococcus aureus (S1 and S2) of different origin. The most active 13-hexylberberine was 8 times more active (against S1) and the same order active (against S2) as kanamycin sulfate. 13-Hexylpalmatine displayed an activity against S. aureus (S1) 4 times greater than that of kanamycin sulfate. The activities of 13-hexylberberine against two types of S. aureus were 64 and 128 times greater than those of the clinically used alkaloid berberine. Additionally two hexyl derivatives possessed antifungal activity.