Novel pyridine-2,4,6-tricarbohydrazide derivatives: Design, synthesis, characterization and in vitro biological evaluation as alpha- and beta-glucosidase inhibitors

作者：Riaz Sadaf; Khan Islam Ullah; Yar Muhammad^*; Ashraf Muhammad; Rehman Tanzeel Ur; Shaukat Ayesha; Jamal Syed Babar; Duarte Vera C M; Alves Maria J

来源：Bioorganic Chemistry, 2014, 57: 148-154.

DOI：10.1016/j.bioorg.2014.10.007

• Diabetes
• alpha-Glucosidase
• beta-Glucosidase
• Pyridine-2,4,6-tricarbohydrazide
• Acarbose
• MMFF94X Solvation

A range of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4h) were synthesized and its biological inhibition towards alpha- and beta-glucosidases was studied. Most of the compounds demonstrate to be active against a-glucosidase, and quite inactive/completely inactive against beta-glucosidase. A number of compounds were found to be more active against alpha-glucosidase than the reference compound acarbose (IC50 38.25 +/- 0.12 mu M); being compound 4d with the p-hydroxy phenyl motive the most active (IC50 20.24 +/- 0.72 mu M). Molecular modeling studies show the interactions of compound 4d with the active site of target alpha-glucosidase kinase.

• 出版日期2014-12