The synthesis and biological activity evaluation of benzenesulfonyl hydrazones is quite frequently encountered in scientific literature. This class of compounds is very interesting due to the wide spectrum of potential applications in the field of medicinal chemistry. The benzenesulfonyl hydrazones possess mainly antibacterial, antifungal, anticancer, antidepressant properties, activity against Alzheimer's disease, insecticidal activity and ability to inhibit the activity of enzymes. This review is an attempt to gather the literature findings on the most promising bioactive benzenesulfonyl hydrazones.