Synthesis, molecular modelling and pharmacological evaluation of novel indole-thiazolidinedione based hybrid analogues as potential pancreatic lipase inhibitors

A series of novel indole-thiazolidinedione hybrid analogues ( to ) were synthesised, characterised and evaluated for their potential Pancreatic Lipase (PL) inhibition. Amongst the screened analogues, was found to be the most active PL inhibitor with an IC of 2.67 µM. Furthermore, enzyme inhibition k...

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Bibliographic Details
Published in:Journal of biomolecular structure & dynamics 2023-12, p.1-20
Main Authors: George, Ginson, Auti, Prashant S, Sengupta, Pracheta, Yadav, Nisha, Paul, Atish T
Format: Article
Language:English
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Summary:A series of novel indole-thiazolidinedione hybrid analogues ( to ) were synthesised, characterised and evaluated for their potential Pancreatic Lipase (PL) inhibition. Amongst the screened analogues, was found to be the most active PL inhibitor with an IC of 2.67 µM. Furthermore, enzyme inhibition kinetics study revealed a competitive mode of inhibition by the analogues. This fact was confirmed fluorescence spectroscopy which further suggested the presence of one binding site for the synthesized analogues. Molecular docking was performed using human PL (PDB ID: 1LPB) and were in agreement with the results (Pearson's  = 0.8355,  
ISSN:0739-1102
1538-0254
DOI:10.1080/07391102.2023.2293255