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<p>Diabetes mellitus remains a major global health challenge, necessitating the search for potent and safer therapeutic agents. In this study, a series of novel pyrrolo-imidazolidinone derivatives (<b>1–10</b>) was designed and synthesized as potential anti-diabetic agents. Structural elucidation was carried out using HREI-MS, <sup>1</sup>H-NMR and <sup>13</sup>C-NMR spectroscopy. The anti-diabetic potential of the compounds was evaluated in vitro against α-amylase and α-glucosidase enzymes. Among the synthesized derivatives, compounds <b>4</b>,<b> 5</b>,<b> and 7</b> exhibited the most potent inhibitory activity, with IC<sub>50</sub> valuesranging between 4.10 ± 0.30 to 2.10 ± 0.10 µM (α-amylase) and 4.80 ± 0.40 to 2.60 ± 0.20 µM (α-glucosidase), surpassing the reference drug acarbose (IC<sub>50</sub> = 4.20 ± 0.60 µM and 5.10 ± 0.10 µM, respectively). In silico studies, including molecular docking, pharmacophore modeling, and ADMET profiling, supported the experimental findings and provided insights into the structural features governing enzyme inhibition and drug-likeness. The results highlight pyrrolo-imidazolidinone derivatives as promising scaffolds for further development of effective anti-glycemic agents.</p>

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Shifting the paradigm of diabetes mellitus therapeutics: synthesis of novel fused pyrrolo-Imidazolidinone derivatives and their kinetic and computational profiling

  • 期刊论文

  • 发表日期：

    2025年9月18日

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  • Shoaib Khan,
  • Tayyiaba Iqbal,
  • Eman Alzahrani,
  • Faez Falah Alshehri,
  • Zafer Saad Al Shehri,
  • Sobhi M. Gomha,
  • Magdi E. A. Zaki,
  • Hamdy Kashtoh

摘要

Diabetes mellitus remains a major global health challenge, necessitating the search for potent and safer therapeutic agents. In this study, a series of novel pyrrolo-imidazolidinone derivatives (1–10) was designed and synthesized as potential anti-diabetic agents. Structural elucidation was carried out using HREI-MS, 1H-NMR and 13C-NMR spectroscopy. The anti-diabetic potential of the compounds was evaluated in vitro against α-amylase and α-glucosidase enzymes. Among the synthesized derivatives, compounds 4, 5, and 7 exhibited the most potent inhibitory activity, with IC50 valuesranging between 4.10 ± 0.30 to 2.10 ± 0.10 µM (α-amylase) and 4.80 ± 0.40 to 2.60 ± 0.20 µM (α-glucosidase), surpassing the reference drug acarbose (IC50 = 4.20 ± 0.60 µM and 5.10 ± 0.10 µM, respectively). In silico studies, including molecular docking, pharmacophore modeling, and ADMET profiling, supported the experimental findings and provided insights into the structural features governing enzyme inhibition and drug-likeness. The results highlight pyrrolo-imidazolidinone derivatives as promising scaffolds for further development of effective anti-glycemic agents.