Herein, condensation of aryl(hetaryl)pyrazole-4-carbaldehydes 1(a-c) with substituted pyrazolones 2(a-d) lead to the corresponding arylidene-pyrazolones 3(a-l) which were tested against α-glucosidase enzyme. The synthesized compounds displayed moderate to good activity. Among these, a coumarin derivative 3k exhibited excellent results (IC 2.10 ± 0.004 µM) in comparison to clinical drug acarbose (IC 37.38 ± 0.12 µM). The ligand-protein interactions were identified through docking and stabilizing energy calculations.
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http://dx.doi.org/10.1016/j.bioorg.2018.02.002 | DOI Listing |
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