One of the most prevailing metabolic disorder diabetes mellitus has become the global health issue that has to be addressed and cured. Different marketed drugs have been made available for the treatment of diabetes but there is still a need of introducing new therapeutic agents that are economical and have lesser or no side effects. The current study deals with the synthesis of indole acrylonitriles (3–23) and the evaluation of these compounds for their potential for α-glucosidase inhibition. The structures of these synthetic molecules were deduced by using different spectroscopic techniques. Acarbose (IC₅₀ = 2.91 ± 0.02 μM) was used as standard in this study and the synthetic molecules (3–23) have shown promising α-glucosidase inhibitory activity. Compounds 4, 8, 10, 11, 14, 18, and 21 displayed superior inhibition of α-glucosidase enzyme in the range of (IC₅₀ = 0.53 ± 0.01–1.36 ± 0.04 μM) as compared to the standard acarbose. Compound 10 (IC₅₀ = 0.53 ± 0.01 μM) was the most effective inhibitor of this library and displayed many folds enhanced activity in contrast to the standard. Molecular docking of synthetic compounds was performed to verify the binding interactions of ligand with the active site of enzyme. This study had identified a number of potential α-glucosidase inhibitors that can be used for further research to identify a potent therapeutic agent against diabetes.

最流行的代谢紊乱糖尿病之一已成为必须解决的全球健康问题。已经提供了不同的市售药物来治疗糖尿病，但是仍然需要引入经济且副作用较小或没有副作用的新治疗剂。目前的研究涉及吲哚丙烯腈的合成（3 - 23），并且这些化合物对潜在的评价α-葡糖苷酶的抑制作用。这些合成分子的结构是通过使用不同的光谱技术推论得出的。阿卡波糖（IC ₅₀  = 2.91±0.02μM）被用作本研究的标准品，合成分子（3 – 23）已经显示出有希望的α-葡萄糖苷酶抑制活性。化合物4，8，10，11，14，18，和21中显示的优异的抑制α葡糖苷酶酶活性的影响的范围内（IC ₅₀  = 0.53±0.01-1.36±0.04μM）相对于标准如阿卡波糖。化合物10（IC ₅₀ = 0.53±0.01μM）是该文库中最有效的抑制剂，与标准品相比，其活性提高了许多倍。进行合成化合物的分子对接以验证配体与酶活性位点的结合相互作用。这项研究确定了许多潜在的α-葡萄糖苷酶抑制剂，可用于进一步研究，以鉴定出有效的抗糖尿病治疗剂。