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  3. Exploiting oxadiazole-sulfonamide hybrids as new structural leads to combat diabetic complications via aldose reductase inhibition

Exploiting oxadiazole-sulfonamide hybrids as new structural leads to combat diabetic complications via aldose reductase inhibition

  • Bioorg Chem. 2020 Jun;99:103852. doi: 10.1016/j.bioorg.2020.103852.
Noman Javid 1,  Rubina Munir 2,  Faryal Chaudhry 3,  Aqeel Imran 4,  Sumera Zaib 5,  Ayesha Muzaffar 3,  Jamshed Iqbal 6
Affiliations

Affiliations

  • 1 Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.
  • 2 Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan. Electronic address: rubina.munir@kinnaird.edu.pk.
  • 3 Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan.
  • 4 Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan.
  • 5 Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan; Department of Biochemistry, Faculty of Life Sciences, University of Central Punjab, Lahore 54590, Pakistan.
  • 6 Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan. Electronic address: drjamshed@cuiatd.edu.pk.
PMID: 32325339 DOI: 10.1016/j.bioorg.2020.103852
Abstract

A series of oxadiazole-sulfonamide hybrids was synthesized through multistep reaction and for the formation of targeted thioethers 6(a-l), a much facile route was adopted through which S-alkylation was successfully carried out at room temperature. These novel thioethers 6(a-l) were later screened against aldehyde reductase (ALR1) and Aldose Reductase (ALR2). Beside the Enzyme inhibition studies, the compounds were also tested against cervical Cancer cell lines (HeLa). The results suggested the significant inhibition pattern towards ALR2, while few compounds were active against ALR1. The synthesized derivatives have shown weak to moderate cytotoxicity. The most potent inhibitors (6b, 6e, 6f and 6l) were selected for molecular docking studies and the binding interactions were reported.

Keywords

Aldose reductase; Cytotoxicity; Docking studies; Oxadiazole-sulfonamides.

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