关键词: Molecular docking Piperazine SAR Sulfonamide Synthesis α-Amylase inhibition

Mesh : Diabetes Mellitus, Type 2 / drug therapy metabolism Dose-Response Relationship, Drug Enzyme Inhibitors / chemical synthesis chemistry pharmacology Humans Hypoglycemic Agents / chemical synthesis chemistry pharmacology Molecular Docking Simulation Molecular Structure Piperazine Piperazines / chemical synthesis chemistry pharmacology Structure-Activity Relationship Sulfonamides / chemical synthesis chemistry pharmacology alpha-Amylases / antagonists & inhibitors metabolism

来  源:   DOI:10.1016/j.ejmech.2017.10.028   PDF(Sci-hub)

Abstract:
Piperazine Sulfonamide analogs (1-19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1-19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC50 = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2.118 ± 0.204 μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.
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