ArticleFuture medicinal chemistry2025
Piperidines as dual inhibitors of tyrosinase and pancreatic lipase:
Article in Future medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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7 authors.
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Abstract
aimsThis study aimed to explore the dual inhibitory potential of a series of piperidine derivatives against tyrosinase and pancreatic lipase. For the first time, these compounds were evaluated concurrently for their inhibitory effects on both enzymes, targeting potential therapeutic applications in hyperpigmentation and obesity-related disorders. MATERIALS AND
methodsA total of eight piperidine-based compounds were synthesized and assessed for in vitro inhibitory activity against mushroom tyrosinase and pancreatic lipase. The most active derivatives underwent kinetic studies to determine the mode of inhibition using Lineweaver-Burk plots. Structure-activity relationship (SAR) analysis was performed to identify key substituents influencing bioactivity. Furthermore, molecular docking, molecular dynamics (MD) simulations, and density functional theory (DFT) calculations were conducted to elucidate the binding interactions and electronic properties associated with inhibition.
resultsAmong the tested compounds, several exhibited significant dual inhibitory activity, with low micromolar IC
conclusionsThese findings reveal, for the first time, that piperidine derivatives possess promising dual inhibitory activity against tyrosinase and pancreatic lipase, supported by both experimental and computational evidence.
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