Human carbonic anhydrase (hCA) isoenzymes are zinc ion‐containing, widespread metalloenzymes and they classically play a role in pH homeostasis maintenance. CA inhibitors suppress the CA activity and their usage has been clinically established as antiglaucoma agents, antiepileptics, diuretics, and in some other disorders. Alzheimer's disease (AD) is a slowly progressive neurodegenerative disorder and a fatal disease of the brain. An advanced method to cure AD includes the strategy to design acetylcholinesterase (AChE) inhibitors. A novel series of pyrrole‐3‐one derivatives containing sulfa drugs (5a–i) were determined to be highly potent inhibitors for AChE and hCA I and hCA II (inhibitory constant [Ki] values are in the range of 6.50 ± 1.02–37.46 ± 4.12 nM, 1.20 ± 0.19–44.21 ± 1.09 nM, and 8.93 ± 1.58–46.86 ± 8.41 nM for AChE, hCA I, and hCA II, respectively). The designed compounds often show a more effective inhibition than the chemicals used as the standard. Among these compounds, 5f was the most effective compound against hCA I, and compound 5e was the most effective compound against hCA II. It was determined that compound 5c was the most effective inhibitor for AChE.