Synthesis and in vitro Biological Evaluation of a Series of Benzothiazole-Sulfonylurea Hybrids as Novel Class of α-Glucosidase Inhibitors

• Published in: Asian journal of chemistry 2024-05, Vol.36 (6), p.1429-1435
• Main Authors: Harunani, Asmaa, Chua, Bryan Ching Seng, Cheong, Jack Seng, Chok, Jia Ying, Nadhirah Azni, Nur Azizah, Santhiran, Sangeetha, Shajahan, Wasmiya, Lai, Xin Yan, Avupati, Vasudeva Rao
• Format: Article
• Language: English
• ISSN: 0970-7077; 0975-427X
• DOI: 10.14233/ajchem.2024.31558

A series of benzothiazole-sulfonylurea hybrids (C1-C9) were synthesized and the molecular structures were characterized using physical (state, colour, melting point) and spectral (FT-IR, 1H NMR, 13C NMR and ESI-Mass) methods. All the compounds were screened for their bioactive potential as antidiabetic agents through α-glucosidase enzyme inhibitory properties at 100 µM concentration. The results were compared with a standard drug, voglibose. The bioassay results revealed that compound C2 was found to be the hit molecule that has exhibited a percentage enzyme inhibition of 49.10%, which is relatively better than that of voglibose at 37.75%. The observed activity is primarily due to the synergistic or addition potential of the pharmacophores benzothiazole and sulfonylurea hybridized into one molecule; the structural analogues of these pharmacophores were earlier reported as α-glucosidase inhibitors.