Synthesis and evaluation of biological activity of novel sulfonylthiourea derivative

Synthesis And Evaluation Of Biological Activity Of Novel Sulfonylthiourea Derivatives Sülfonilthiourea compounds are of great interest in medicinal chemistry due to their pharmacological activities. In this study, 4-bromobenzenesulfonamide was selected as the starting material. The 4-bromo-N-(4-substituted-phenylcarbamoyl) benzenesulfonamide derivatives were synthesized by the reaction of 4-bromobenzenesulfonamide with isothiocyanate in dry acetone in the presence of potassium carbonate. After the purity of the compounds was confirmed by TLC, their structures were elucidated through elemental analysis and spectral data. The antioxidant activity of the synthesized 13 compounds was evaluated using ABTS+, DPPH, CUPRAC, β-carotene/linoleic acid assays. Their antidiabetic activity was assessed based on α-amylase and α-glucosidase inhibition assays, while their anticholinesterase activity was determined against acetylcholinesterase, butyrylcholinesterase enzymes. Additionally, their tyrosinase inhibition activity was investigated. Compounds 1, 3, 7, 9, 10 and 13 exhibited the most potent antioxidant activity. Among the antidiabetic tests, none of the compounds showed activity in the α-amylase inhibition assay, while compounds 4, 11 and 13 demonstrated significant α-glucosidase inhibitory activity, surpassing the positive standard acarbose. Moreover, compounds 4, 5, 7, 8, 9, 10, 11, and 12 exhibited superior tyrosinase inhibition activity compared to the positive standard kojic acid.