4.2 Article

Synthesis, Antioxidant and Some Enzyme Inhibition Activities of New Sulfonyl Hydrazones and their Molecular Docking Simulations

Journal

PHARMACEUTICAL CHEMISTRY JOURNAL
Volume 56, Issue 4, Pages 559-569

Publisher

SPRINGER
DOI: 10.1007/s11094-022-02674-3

Keywords

sulfonyl hydrazine; antioxidant; anticholinesterase; tyrosinase; urease; molecular docking

Funding

  1. Cankyry Karatekin University Scientific Research Projects Governing Unit (BAPYB) [YM0150219B14]

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In this study, a series of new sulfonyl hydrazones were synthesized and evaluated for their antioxidant and enzyme inhibitory activities. Molecular docking analysis was performed to understand the inhibitory mechanism at the molecular level. Compound 8 showed the most active AChE activity, while compounds 3, 4, 5, 6, 7, and 8 exhibited better BChE and tyrosinase inhibitory activities compared to the standard drug galantamine.
In this work, a series of new sulfonyl hydrazones were synthesized and screened for antioxidant and anticholinesterase, tyrosinase and urease enzyme inhibition activities. In addition, molecular docking study was applied to better understand the inhibitory mechanism at the molecular level. Further, bioavailability of the synthesized compounds is considered in terms of the Lipinski rule and the design of their pharmacokinetic and pharmacodynamic properties is found reliable. In the AChE activity assay results, compound 8 was the most active one, while being less active than galantamine that was used as the standard drug. In the BChE activity testing of sulfonyl hydrazone derivatives (1-8), , compounds 3, 4, 5, 6, 7 and 8 were the most active drugs and showed much better activity than galantamine used as the standard. Compounds 8, 5 and 4 showed the best tyrosinase inhibitory activity with IC50 values of 9.75 +/- 0.23, 13.18 +/- 0.67 and 16.29 +/- 0.73 mM, respectively.

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