| Summary: | Sulfonyl drugs are widely used to treat various types of diseases, in which sultones have several desirable properties that have led to their increased use, including improving its simple and effective synthetic methods and/or potentially enhancing potency of drugs. This review focuses on the recent progress in typical synthesis of sultones and the latest developments in various therapeutic applications, including carbonic anhydrase inhibitory activity, HIV-I and HIV-II inhibitory activity, human cytomegalovirus inhibitory activity, and cholinesterase inhibitory activity and their structure–activity relationship. We hope that this review will encourage medicinal chemists to consider the potential benefits to incorporating sultone scaffold into future drug discovery.
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