New pyridine-based imines to treat diabetes mellitus targeting α-glucosidase: in silico design, docking and in vitro biological evaluation

Amit Patel , Neha D. Kawathekar , Gaurav Jain

α-glucosidase inhibition, Acarbose, Pyridine, Imines, Molecular docking

A novel series of pyridine-based imines were rationally designed and synthesized as anti-diabetic agents. Out of all the synthesized compounds, 3 compounds were selected and were screened for possible α-glucosidase inhibitory potential at two concentrations (1uM and 10Um) wherein they exhibited alpha-glucosidase inhibition in the range of 21.23%-36.67% at 1uM concentration and 38.42%-52.31% at 10uM in comparison with acarbose as the positive control which showed an inhibition of 53.34% at 1uam concentration and of 72.56% at 10uM concentration. VR3 was the most potent derivative, bearing 4-Chloro moiety. Additionally, the molecular docking of all derivatives was performed to get an insight into the binding mode of these derivatives within the active site of the enzyme. In silico assessments exhibited that all the designed compounds were well occupied in the binding pocket of the enzyme through favorable interactions with various amino acid residues in the active site, correlating to the experimental results.

Published Paper   E-Certificate

"New pyridine-based imines to treat diabetes mellitus targeting α-glucosidase: in silico design, docking and in vitro biological evaluation", IJSDR - International Journal of Scientific Development and Research (www.IJSDR.org), ISSN:2455-2631, Vol.8, Issue 3, page no.723 - 730, March-2023, Available :https://ijsdr.org/papers/IJSDR2303117.pdf

Volume 8 Issue 3, March-2023

Pages : 723 - 730

Paper Reg. ID: IJSDR_204495

Published Paper Id: IJSDR2303117

Downloads: 000347213

Research Area: Pharmacy

Country: Sahodaya Convt., Badoli Hauj, Depalpur, Indore, M., Madhya Pradesh, India

Published Paper PDF: https://ijsdr.org/papers/IJSDR2303117

Published Paper URL: https://ijsdr.org/viewpaperforall?paper=IJSDR2303117

ISSN: 2455-2631 | IMPACT FACTOR: 9.15 Calculated By Google Scholar | ESTD YEAR: 2016

An International Scholarly Open Access Journal, Peer-Reviewed, Refereed Journal Impact Factor 9.15 Calculate by Google Scholar and Semantic Scholar | AI-Powered Research Tool, Multidisciplinary, Monthly, Multilanguage Journal Indexing in All Major Database & Metadata, Citation Generator

Publisher: IJSDR(IJ Publication) Janvi Wave

This work is licensed under a Creative Commons Attribution 4.0 International License and The Open Definition