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<p>The current research is associated with the green synthesis of a series of polyhydroxy-conjugated piperidine derivatives (<b>4a-f</b>) and screened for antiglycation activity. Microwave-assisted method, which offers a sustainable, energy-efficient alternative to conventional synthesis. Compound <b>4f</b> was found to most potent α-glucosidase inhibitor (IC<sub>50</sub> = 47.65 ± 0.88 µM), which was even more active than rutin (IC<sub>50</sub> = 72.66 ± 1.45 µM) and significantly inhibited the formation of advanced glycation end products, fructosamine (IC<sub>50</sub> = 46.67 ± 2.02 µM), thiol oxidation (IC<sub>50</sub> = 93.50 ± 7.12 µM), and congo red binding (IC<sub>50</sub> = 37.00 ± 1.52 µM). The structure-activity relationship (SAR) analysis revealed that the electron-donating substituents completely increased bioactivity. The binding affinity of compound <b>4f</b> (-207.035&#xa0;kcal/mol) towards the 3A4A enzyme of pdb (ID: 3A4A) was also further supported by the molecular docking simulation in comparison to rutin. Overall, these findings support the promise of the green-synthesized polyhydroxy-conjugated piperidine derivatives as promising compounds in the combined management of diabetes.</p> Graphical Abstract <p></p>

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Microwave-Assisted Synthesis of Some Novel Polyhydroxy Piperidine Compounds for Antiglycation Activity: In-Vitro and In-Silico Validation

  • 期刊论文

  • 发表日期：

    2026年1月19日

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  • Anju Daharia,
  • Alok Singh Thakur,
  • Lokkanya Dewangan

摘要

The current research is associated with the green synthesis of a series of polyhydroxy-conjugated piperidine derivatives (4a-f) and screened for antiglycation activity. Microwave-assisted method, which offers a sustainable, energy-efficient alternative to conventional synthesis. Compound 4f was found to most potent α-glucosidase inhibitor (IC50 = 47.65 ± 0.88 µM), which was even more active than rutin (IC50 = 72.66 ± 1.45 µM) and significantly inhibited the formation of advanced glycation end products, fructosamine (IC50 = 46.67 ± 2.02 µM), thiol oxidation (IC50 = 93.50 ± 7.12 µM), and congo red binding (IC50 = 37.00 ± 1.52 µM). The structure-activity relationship (SAR) analysis revealed that the electron-donating substituents completely increased bioactivity. The binding affinity of compound 4f (-207.035 kcal/mol) towards the 3A4A enzyme of pdb (ID: 3A4A) was also further supported by the molecular docking simulation in comparison to rutin. Overall, these findings support the promise of the green-synthesized polyhydroxy-conjugated piperidine derivatives as promising compounds in the combined management of diabetes.

Graphical Abstract