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INTERNATIONAL JOURNAL OF SCIENTIFIC DEVELOPMENT AND RESEARCH International Peer Reviewed & Refereed Journals, Open Access Journal ISSN Approved Journal No: 2455-2631 | Impact factor: 8.15 | ESTD Year: 2016 open access , Peer-reviewed, and Refereed Journals, Impact factor 8.15 |
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| Paper Title: | New pyridine-based imines to treat diabetes mellitus targeting α-glucosidase: in silico design, docking and in vitro biological evaluation |
| Authors Name: | Amit Patel , Neha D. Kawathekar , Gaurav Jain |
| Unique Id: | IJSDR2303117 |
| Published In: | Volume 8 Issue 3, March-2023 |
| Abstract: | 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. |
| Keywords: | α-glucosidase inhibition, Acarbose, Pyridine, Imines, Molecular docking |
| Cite Article: | "New pyridine-based imines to treat diabetes mellitus targeting α-glucosidase: in silico design, docking and in vitro biological evaluation", International Journal of Science & Engineering Development Research (www.ijsdr.org), ISSN:2455-2631, Vol.8, Issue 3, page no.723 - 730, March-2023, Available :http://www.ijsdr.org/papers/IJSDR2303117.pdf |
| Downloads: | 000337077 |
| Publication Details: | Published Paper ID: IJSDR2303117 Registration ID:204495 Published In: Volume 8 Issue 3, March-2023 DOI (Digital Object Identifier): Page No: 723 - 730 Publisher: IJSDR | www.ijsdr.org ISSN Number: 2455-2631 |
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