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<p>A series of imine derivatives of isatin 4(a–e), 5(a–e), 6(a–b) were synthesized using aliphatic hydrazides and substituted isatins. Synthesized products were analyzed by spectroanalytical techniques and evaluated for urease and <i>α</i>-glucosidase inhibition activities. Compounds 3a, 3b, 4b, 5a, 5b, 5c and 6a with an IC<sub>50</sub> values 50.40 ± 0.21, 46.19 ± 0.21, 46.03 ± 1.22, 43.33 ± 0.62, 50.67 ± 0.13, 45.78 ± 3.53, 50.34 ± 1.92 [µM] respectively exhibited excellent urease inhibition results compared to the standard [24.14&#xa0;µM]. However with respect to α-glucosidase inhibition activity, the compounds 3b, 4a, 5a, 5b, and 5c with IC<sub>50</sub> values 133.08 ± 0.24, 162.15 ± 0.32, 128.56 ± 2.42, 136.70 ± 3.22 and 145.33 ± 0.32 [µM] respectively showed good inhibition. Results were also supported by docking studies.</p>

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Synthesis, enzyme inhibition and docking studies of isatin derivatives from aliphatic esters

  • 期刊论文

  • 发表日期：

    2025年7月27日

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  • Rifhat Sultana,
  • Obaid-ur-Rahman Abid,
  • Saira Bibi,
  • Mohsin Ali,
  • Syed Maeen Badshah,
  • Shoaib Khan,
  • Zaheed Ahmed

摘要

A series of imine derivatives of isatin 4(a–e), 5(a–e), 6(a–b) were synthesized using aliphatic hydrazides and substituted isatins. Synthesized products were analyzed by spectroanalytical techniques and evaluated for urease and α-glucosidase inhibition activities. Compounds 3a, 3b, 4b, 5a, 5b, 5c and 6a with an IC50 values 50.40 ± 0.21, 46.19 ± 0.21, 46.03 ± 1.22, 43.33 ± 0.62, 50.67 ± 0.13, 45.78 ± 3.53, 50.34 ± 1.92 [µM] respectively exhibited excellent urease inhibition results compared to the standard [24.14 µM]. However with respect to α-glucosidase inhibition activity, the compounds 3b, 4a, 5a, 5b, and 5c with IC50 values 133.08 ± 0.24, 162.15 ± 0.32, 128.56 ± 2.42, 136.70 ± 3.22 and 145.33 ± 0.32 [µM] respectively showed good inhibition. Results were also supported by docking studies.