Abstract
A series of 6 novel ester derivatives 2–7 of natural product geodin 1 were designed and semi-synthesized through one mild step reaction with high yield. Compounds 2–7 showed strong inhibitory activities against Staphylococcus aureus in the range of 2.35–9.41 μM. Compounds 4 and 7 showed very strong inhibitory activities against antifouling bacteria Aeromonas salmonicida with MICs of 2.42 μM and 4.56 μM respectively. Most notably compounds 3–7 showed potent antifungal activities against Candida albicans in the range of 0.59–2.44 μM. Particularly, compound 3 showed the highest antifungal activity against C. albicans with a MIC value of 0.59 μM. The preliminary structure activity relationship of these derivatives showed that replacement of 4-OH group with benzoyl substituents could enhance the antibacterial and antifungal activities of geodin 1.
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