New Hybrid Hydrazinyl Thiazole Substituted Chromones: As Potential α-Amylase Inhibitors and Radical (DPPH & ABTS) Scavengers View Full Text


Ontology type: schema:ScholarlyArticle      Open Access: True


Article Info

DATE

2017-12

AUTHORS

Uzma Salar, Khalid Mohammed Khan, Sridevi Chigurupati, Muhammad Taha, Abdul Wadood, Shantini Vijayabalan, Mehreen Ghufran, Shahnaz Perveen

ABSTRACT

Current research is based on the identification of novel inhibitors of α-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 α-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 α-amylase enzyme. More... »

PAGES

16980

Identifiers

URI

http://scigraph.springernature.com/pub.10.1038/s41598-017-17261-w

DOI

http://dx.doi.org/10.1038/s41598-017-17261-w

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1093099596

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/29209017


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42 schema:description Current research is based on the identification of novel inhibitors of α-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, <sup>1</sup>H-NMR and <sup>13</sup>C-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 α-amylase inhibitory, DPPH and ABTS radical scavenging activities. All compounds showed good inhibition potential in the range of IC<sub>50</sub> = 2.186-3.405 µM as compared to standard acarbose having IC<sub>50</sub> value of 1.9 ± 0.07 µM. It is worth mentioning that compounds were also demonstrated good DPPH (IC<sub>50</sub> = 0.09-2.233 µM) and ABTS (IC<sub>50</sub> = 0.584-3.738 µM) radical scavenging activities as compared to standard ascorbic acid having IC<sub>50</sub> = 0.33 ± 0.18 µM for DPPH and IC<sub>50</sub> = 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 α-amylase enzyme.
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