| Sumario: | Altholactone exhibited the anti-fungal activity with a high MIC value of 128 μg ml−1againstCryptococcus neoformansandSaccharomyces cerevisiae. Fifteen ester derivatives of altholactone1–15were modified by esterification and their structures were confirmed by spectroscopic methods. Most of the ester derivatives exhibited stronger anti-fungal activities than that of the precursor altholactone. 3-Bromo- and 2,4-dichlorobenzoates (7and15) exhibited the lowest minimal inhibitory concentration (MIC) values againstC.neoformansat 16 μg ml−1,while the 4-bromo-, 4-iodo-, and 1-bromo-3-chlorobenzoates (11–13) displayed potent activity againstS. cerevisiaewith MIC values of 1 μg ml−1. In conclusion, this analysis indicates that the anti-fungal activity of altholactone is enhanced by addition of halogenated benzoyl group to the 3-OH group.
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