| Literature DB >> 29454828 |
Faryal Chaudhry1, Sadia Naureen2, Shahnaz Choudhry3, Rahila Huma4, Muhammad Ashraf5, Mariya Al-Rashida6, Bakhat Jahan5, Masooma Hyder Khan4, Farah Iqbal4, Munawar Ali Munawar7, Misbahul Ain Khan8.
Abstract
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 (IC50 2.10 ± 0.004 µM) in comparison to clinical drug acarbose (IC50 37.38 ± 0.12 µM). The ligand-protein interactions were identified through docking and stabilizing energy calculations.Entities:
Keywords: Antipyrine; Arylidenes; Coumarins; Enzyme Inhibitor; Knoevenagel condensations
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Substances:
Year: 2018 PMID: 29454828 DOI: 10.1016/j.bioorg.2018.02.002
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275