Chiang Mai Journal of Science

Diabetes mellitus is a severe disease world over which is caused due to the insufficient or lack of insulin production that results in an increase in blood level. Use of various synthetic drugs is a key to lower the glucose level which act as inhibitors of enzyme such as α-glucosidase which is responsible for the glucose production. In order to explore novel and more potent α-glucosidase inhibitors, we evaluated thirteen 1,2-benzothiazine derivatives for their in silico α-glucosidase inhibitory potential and as a result six compounds (1, 3, 4, 8, 9 and 10) with low rmsd values showed good binding energies and interactions with the active site residues. These six best compounds were also subjected to the in vitro alpha glucosidase inhibition and a good agreement was found between the results. Compound 1, 8 and 9 showed excellent results having IC₅₀ values of 5.9, 7.8 and 3.9 μM respectively, even less than the standard acarbose (IC₅₀ = 38.3 μM). These derivatives were also proved more potent antidiabetic agents compared to some previously reported heterocyclic compounds. Hence, the presented derivatives may be used as lead candidates to cure diabetes