A series of simple N-arylbenzenesulfonyl histamine derivatives were prepared and screened against α-glucosidase. Inhibition was in the micromolar range for several N^α,N^τ-di-arylsulfonyl compounds, with N^α,N^τ-di-4-trifluorobenzenesulfonyl histamine (IId) being the best inhibitor. Compound IId is a reversible and competitive α-glucosidase inhibitor, and presented good selectivity with respect to other target enzymes, including β-glucosidase and α-amylase, and interesting predicted physicochemical properties. Docking studies have been run to postulate ligand–enzyme interactions to account for the experimental results. In vivo, compound IId produced a similar hypoglycemic effect to acarbose with half of its dose.

中文翻译：

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芳基磺酰基组胺衍生物作为强效和选择性 α-葡萄糖苷酶抑制剂

制备了一系列简单的N-芳基苯磺酰基组胺衍生物，并针对 α-葡萄糖苷酶进行了筛选。几种N ^α , N ^τ -二芳基磺酰基化合物的抑制作用在微摩尔范围内，其中N ^α , N ^τ -二-4-三氟苯磺酰基组胺 ( IId ) 是最好的抑制剂。化合物IId是一种可逆的竞争性α-葡萄糖苷酶抑制剂，对其他靶酶具有良好的选择性，包​​括β-葡萄糖苷酶和α-淀粉酶，以及有趣的预测物理化学性质。已经进行了对接研究以假设配体-酶相互作用来解释实验结果。在体内，化合物IId产生与阿卡波糖相似的降血糖作用，其剂量减半。