α-Glucosidase inhibition is considered as an effective strategy for the treatment of diabetes mellitus. Currently, three α-glucosidase inhibitors are being used as drugs; Acarbose, Voglibose and Miglitol. The side effects of these drugs are forcing researchers to search for new and effective molecules. In this research work, novel 1,2,3-benzotriazin-4(3H)-one sulfonamides were synthesized and investigated for their α-glucosidase inhibition activity. 2,4,6-Trichloro-1,3,5-triazine: N,N-dimethylformamide (TCT : DMF) adduct have been utilized for the direct synthesis of targeted sulfonamides. All reactions were performed at room temperature under mild conditions. In-vitro enzyme inhibition studies led us to discover many potent inhibitors demonstrating good to excellent activity. The compound 5c with dimethyl substituent was found to be a more potent inhibitor than acarbose with the IC₅₀ value of 29.75 ± 0.14 μM. Compounds 5a, 5b, 5d, 5e, 5f, and 5m showed good inhibition results with IC₅₀ value 31.97 ± 0.03, 33.24 ± 0.01, 33.76 ± 1.05, 35.98 ± 0.03, 30.87 ± 0.51, and 37.24 ± 0.04 µM respectively. Further structure activity relationship was analyzed by molecular docking studies.

α-葡萄糖苷酶抑制被认为是治疗糖尿病的有效策略。目前，三种α-葡萄糖苷酶抑制剂被用作药物；阿卡波糖、伏格列波糖和米格列醇。这些药物的副作用迫使研究人员寻找新的有效分子。在这项研究工作中，合成了新型 1,2,3-benzotriazin-4(3 H )-one 磺胺类药物，并研究了它们的α -葡萄糖苷酶抑制活性。2,4,6-三氯-1,3,5-三嗪：N,N-二甲基甲酰胺 (TCT : DMF) 加合物已用于直接合成靶向磺胺类药物。所有反应均在温和条件下于室温下进行。体外酶抑制研究使我们发现了许多有效的抑制剂，显示出良好的活性。发现具有二甲基取代基的化合物5c是比阿卡波糖更有效的抑制剂，IC ₅₀值为 29.75 ± 0.14 μM。化合物5a、5b、5d、5e、5f和5m显示出良好的抑制效果，IC ₅₀值分别为 31.97 ± 0.03、33.24 ± 0.01、33.76 ± 1.05、35.98 ± 0.03、30.87 ± 0.51 和 37.24 ± 0.04 µM。通过分子对接研究分析了进一步的结构活性关系。