Department of Chemistry, GC University, Lahore 54000, Pakistan.
Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan.
Bioorg Chem. 2014 Dec;57:148-154. doi: 10.1016/j.bioorg.2014.10.007. Epub 2014 Nov 6.
A range of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4h) were synthesized and its biological inhibition towards α- and β-glucosidases was studied. Most of the compounds demonstrate to be active against α-glucosidase, and quite inactive/completely inactive against β-glucosidase. A number of compounds were found to be more active against α-glucosidase than the reference compound acarbose (IC50 38.25±0.12μM); being compound 4d with the p-hydroxy phenyl motive the most active (IC50 20.24±0.72μM). Molecular modeling studies show the interactions of compound 4d with the active site of target α-glucosidase kinase.
一系列新型吡啶 2,4,6-三羧酸二酰肼衍生物（4a-4h）被合成，并研究了其对α-和β-葡萄糖苷酶的生物抑制作用。大多数化合物对α-葡萄糖苷酶表现出活性，而对β-葡萄糖苷酶则几乎没有活性/完全没有活性。一些化合物被发现比参考化合物阿卡波糖（IC50 38.25±0.12μM）对α-葡萄糖苷酶更具有活性；具有对羟基苯基动力的化合物 4d 是最具活性的（IC50 20.24±0.72μM）。分子模拟研究表明化合物 4d 与靶标α-葡萄糖苷酶激酶的活性位点相互作用。
