Synthesis of new indazole based dual inhibitors of α-glucosidase and α-amylase enzymes, their in vitro, in silico and kinetics studies.

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ID: 81927
2020
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Abstract
The current study describes the discovery of novel inhibitors of α-glucosidase and α-amylase enzymes. For that purpose, new hybrid analogs of N-hydrazinecarbothioamide substituted indazoles 4-18 were synthesized and fully characterized by EI-MS, FAB-MS, HRFAB-MS, H-, and C NMR spectroscopic techniques. Stereochemistry of the imine double bond was established by NOESY measurements. All derivatives 4-18 with their intermediates 1-3, were evaluated for in vitro α-glucosidase and α-amylase enzyme inhibition. It is worth mentioning that all synthetic compounds showed good inhibition potential in the range of 1.54 ± 0.02-4.89 ± 0.02 µM for α-glucosidase and for α-amylase 1.42 ± 0.04-4.5 ± 0.18 µM in comparison with the standard acarbose (IC value of 1.36 ± 0.01 µM). In silico studies were carried out to rationalize the mode of binding interaction of ligands with the active site of enzymes. Moreover, enzyme inhibitory kinetic characterization was also performed to understand the mechanism of enzyme inhibition.
Reference Key
rafique2020synthesisbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Rafique, Rafaila;Khan, Khalid Mohammed;Arshia, ;Kanwal, ;Chigurupati, Sridevi;Wadood, Abdul;Rehman, Ashfaq Ur;Karunanidhi, Arunkumar;Hameed, Shehryar;Taha, Muhammad;Al-Rashida, Mariya;
Journal Bioorganic chemistry
Year 2020
DOI
S0045-2068(19)30513-9
URL
Keywords
α-glucosidase hyperglycemia α-amylase carbothioamide indazole

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