Tryptanthrin (T) and 13 of its derivatives (T2NH 2 , T2Cl, T2Br, T2NO 2 , T8OMe, T8Me, T8F, T8Br, T8NO 2 , T2NH 2 8OMe, T2NH 2 8NO 2 , T2Br8Br, and T2NO 2 8NO 2) were synthesized, and their antimicrobial activities against a gram-positive bacterium (methicillin-resistant Staphylococcus aureus, MRSA) and a fungus (Malassezia furfur) were investigated. The antibacterial and antifungal activities were influenced by the substituents on tryptanthrin, with halogen-substituted tryptanthrin derivatives (T2Cl, T2Br, T8F, T8Br, and T2Br8Br) showing the highest potency against MRSA and M. furfur.

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We assayed biologically significant isoprenoids for antibacterial and antifungal activities. Isoprenoids varied widely with respect to their growth inhibitory activities towards Gram-positive and Gram-negative bacteria and fungal species. Of particular interest was the finding that geraniol acted as a broad spectrum of antibiotic, and significantly inhibited the growth of Gram-positive Staphylococcus aureus 209P and methicillin resistant S. aureus 834, Gram-negative Escherichia coli IFO-3806, and Shigella sonnei, as well as the fungus Trichopyton sp. Farnesol inhibited S. aureus strains 209P and 834 to a greater extent than did geraniol, but did not detectably inhibit Gram-negative bacteria.

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