New Hybrid Hydrazinyl Thiazole Substituted Chromones: As Potential ?-Amylase Inhibitors and Radical (DPPH & ABTS) Scavengers.

ABSTRACT: Current research is based on the identification of novel inhibitors of ?-amylase enzyme. For that purpose, new hybrid molecules of hydrazinyl thiazole substituted chromones 5-27 were synthesized by multi-step reaction and fully characterized by various spectroscopic techniques such as EI-MS, HREI-MS, 1H-NMR and 13C-NMR. Stereochemistry of the iminic bond was confirmed by NOESY analysis of a representative molecule. All compounds 5-27 along with their intervening intermediates 1-4, were screened for in vitro ?-amylase inhibitory, DPPH and ABTS radical scavenging activities. All compounds showed good inhibition potential in the range of IC50?=?2.186-3.405?µM as compared to standard acarbose having IC50 value of 1.9?±?0.07?µM. It is worth mentioning that compounds were also demonstrated good DPPH (IC50?=?0.09-2.233?µM) and ABTS (IC50?=?0.584-3.738?µM) radical scavenging activities as compared to standard ascorbic acid having IC50?=?0.33?±?0.18?µM for DPPH and IC50?=?0.53?±?0.3?µM for ABTS radical scavenging activities. In addition to that cytotoxicity of the compounds were checked on NIH-3T3 mouse fibroblast cell line and found to be non-toxic. In silico studies were performed to rationalize the binding mode of compounds (ligands) with the active site of ?-amylase enzyme.

SUBMITTER: Salar U 

PROVIDER: S-EPMC5717224 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature