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<p>In the present work, new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives <b>12a-o</b> were assigned as potent anti-diabetic agents that targeting α-glucosidase and α-amylase as two important targets in treatment of type 2 diabetes. General scaffold of these compounds was designed based on the reported potent α-glucosidase and α-amylase inhibitors and derivation was performed in acetamide moiety. In vitro evaluation of the new compounds <b>12a-o</b> demonstrated that most of the synthesized compounds were more potent than standard inhibitor acarbose against α-glucosidase while all these new compounds were more potent than acaerbose against α-amylase. The most potent compound against both studied enzymes was compound <b>12n</b> that was a 4-fluorophenylacetamide derivative. This compound was 5 and 23.8 folds more potent than acarbose against α-glucosidase and α-amylase, respectively, and with excellent binding energies in comparison to acarbose attached to active sites of these enzymes. Molecular dynamics and pharmacokinetic studies of compound <b>12n</b> was also performed.</p>

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Introduction of new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives as new α-glucosidase and α-amylase inhibitors

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年8月26日

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  • Parisa Nikfar,
  • Somaye Karimian,
  • Sajedeh Safapoor,
  • Milad Noori,
  • Navid Dastyafteh,
  • Seyedeh Niloufar Ghafouri,
  • Maryam Mohammadi-Khanaposhtani,
  • Bagher Larijani,
  • Parham Taslimi,
  • Mohammad Mahdavi

摘要

In the present work, new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives 12a-o were assigned as potent anti-diabetic agents that targeting α-glucosidase and α-amylase as two important targets in treatment of type 2 diabetes. General scaffold of these compounds was designed based on the reported potent α-glucosidase and α-amylase inhibitors and derivation was performed in acetamide moiety. In vitro evaluation of the new compounds 12a-o demonstrated that most of the synthesized compounds were more potent than standard inhibitor acarbose against α-glucosidase while all these new compounds were more potent than acaerbose against α-amylase. The most potent compound against both studied enzymes was compound 12n that was a 4-fluorophenylacetamide derivative. This compound was 5 and 23.8 folds more potent than acarbose against α-glucosidase and α-amylase, respectively, and with excellent binding energies in comparison to acarbose attached to active sites of these enzymes. Molecular dynamics and pharmacokinetic studies of compound 12n was also performed.