A series of thirty-four diarylpentanoids derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity. Eleven compounds (19, 20, 21, 24, 27, 28, 29, 31, 32, 33 and 34) were found to significantly inhibit α-glucosidase in which compounds 28, 31 and 32 demonstrated the highest activity with IC₅₀ values ranging from 14.1 to 15.1 µM. Structure-activity comparison shows that multiple hydroxy groups are essential for α-glucosidase inhibitory activity. Meanwhile, 3,4-dihydroxyphenyl and furanyl moieties were found to be crucial in improving α-glucosidase inhibition. Molecular docking analyses further confirmed the critical role of both 3,4-dihydroxyphenyl and furanyl moieties as they bound to α-glucosidase active site in different mode. Overall result suggests that diarylpentanoids with both five membered heterocyclic ring and polyhydroxyphenyl moiety could be a new lead design in the search of novel α-glucosidase inhibitor.

合成了一系列的三十二个二芳基戊烷衍生物，并评估了它们的α-葡萄糖苷酶抑制活性。11种化合物（19，20，21，24，27，28，29，31，32，33和34）被发现显著抑制α葡糖苷酶，其中的化合物28，31和32表现出最高的活性，IC ₅₀值范围从14.1到15.1 µM。结构活性比较表明，多个羟基对于α-葡糖苷酶抑制活性是必不可少的。同时，发现3，4-二羟基苯基和呋喃基部分对于改善α-葡糖苷酶抑制作用至关重要。分子对接分析进一步证实了3,4-二羟基苯基和呋喃基部分在以不同方式与α-葡萄糖苷酶活性位点结合时都起着至关重要的作用。总体结果表明，具有五元杂环和多羟基苯基部分的二芳基戊烷可能是寻找新型α-葡萄糖苷酶抑制剂的一种新的先导设计。