In the present work, a new series of 14 novel phthalimide-benzenesulfonamide derivatives 4a–n were synthesized, and their inhibitory activity against yeast α-glucosidase was screened. The obtained results indicated that most of the newly synthesized compounds showed prominent inhibitory activity against α-glucosidase. Among them, 4-phenylpiperazin derivative 4m exhibited the strongest inhibition with the IC50 value of 52.2 ± 0.1 µM. Enzyme kinetic study of compound 4m proved that its inhibition mode was competitive and Ki value of this compound was calculated to be 52.7 µM. In silico induced fit docking and molecular dynamics studies were performed to further investigate the interaction, orientation, and conformation of the target compounds over the active site of α-glucosidase. Obtained date of these studies demonstrated that our new compounds interacted as well with the α-glucosidase active site with the acceptable binding energies. Furthermore, in silico druglikeness/ADME/Toxicity studies of compound 4m were performed and predicted that this compound is druglikeness and has good ADME and toxicity profiles.

Background: In this paper, a novel catalyst is synthesized and characterized by immobilization of copper onto imidazolylpyridine modified super paramagnetic iron oxide nanoparticles (SPION). Methods: The catalyst is characterized by several methods, including TEM, SEM, ICP, DLS, and VSM. The catalytic activity of the catalyst is evaluated in the synthesis of thiosolfunamide. The synthesized catalyst showed very good activity in the mentioned reaction and showed very good performance for the synthesis of the desired products in high isolated yields. Results: For the synthesis of the products, sequential transformations enable the facile synthesis of complex target molecules from simple building blocks in a single preparative step. Conclusion: Using terminal alkynes and sulfonyl azides as starting materials, the reaction can be performed with high yield using water and ethanol as the reaction green solvent. The reusability of the catalyst was tested and the results proved the high reusability of the catalyst.