dc.contributor.author | Saleem, Faiza | |
dc.contributor.author | Khan, Khalid Mohammed | |
dc.contributor.author | Ullah, Nisar | |
dc.contributor.author | Özil, Musa | |
dc.contributor.author | Baltaş, Nimet | |
dc.contributor.author | Hameed, Shehryar | |
dc.contributor.author | Salar, Uzma | |
dc.contributor.author | Wadood, Abdul | |
dc.contributor.author | Rehman, Ashfaq Ur | |
dc.contributor.author | Kumar, Mukesh | |
dc.contributor.author | Taha, Muhammad | |
dc.contributor.author | Haider, Syed Moazzam | |
dc.date.accessioned | 2022-11-24T08:06:22Z | |
dc.date.available | 2022-11-24T08:06:22Z | |
dc.date.issued | 2022 | en_US |
dc.identifier.citation | Saleem, F., Khan, K. M., Ullah, N., Özil, M., Baltaş, N., Hameed, S., Salar, U., Wadood, A., Rehman, A. U., Kumar, M., Taha, M., & Haider, S. M. (2022). Bioevaluation of synthetic pyridones as dual inhibitors of α-amylase and α-glucosidase enzymes and potential antioxidants. Archiv der Pharmazie, e2200400. Advance online publication. https://doi.org/10.1002/ardp.202200400 | en_US |
dc.identifier.issn | 0365-6233 | |
dc.identifier.issn | 1521-4184 | |
dc.identifier.uri | https://doi.org/10.1002/ardp.202200400 | |
dc.identifier.uri | https://hdl.handle.net/11436/7142 | |
dc.description.abstract | Herein, a library of novel pyridone derivatives 1-34 was designed, synthesized, and evaluated for alpha-amylase and alpha-glucosidase inhibitory as well as antioxidant activities. Pyridone derivatives 1-34 were synthesized via a one-pot multi-component reaction of variously substituted aromatic aldehydes, acetophenone, ethyl cyanoacetate, and ammonium acetate in absolute ethanol. Synthetic compounds 1-34 were structurally characterized by different spectroscopic techniques. Most of the tested compounds showed more promising inhibition potential than the standard acarbose (IC50 = 14.87 +/- 0.16 mu M) but compounds 13 and 12 were found to be the most potent compounds with IC50 values of 9.20 +/- 0.14 mu M and 3.05 +/- 0.18 mu M against alpha-amylase and alpha-glucosidase enzymes, respectively. Compounds 1-34 also displayed moderate antioxidant potential in the range of IC50 = 96.50 +/- 0.45 to 189.98 +/- 1.00 mu M in comparison to the control butylated hydroxytoluene (BHT) (IC50 = 66.50 +/- 0.36 mu M), in DPPH radical scavenging activities. Additionally, all synthetic derivatives were subjected to a molecular docking study to investigate the interaction details of compounds 1-34 (ligands) with the active site of enzymes (receptors). These results indicate that the newly synthesized pyridone class may serve as promising lead candidates for controlling diabetes mellitus and as antioxidants. | en_US |
dc.description.sponsorship | Higher Education Commission of Pakistan SHEC/SRSP/Med-3/15/2021-2 | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Wiley | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Enzyme inhibition | en_US |
dc.subject | Molecular modeling | en_US |
dc.subject | Synthesis | en_US |
dc.title | Bioevaluation of synthetic pyridones as dual inhibitors of alpha-amylase and alpha-glucosidase enzymes and potential antioxidants | en_US |
dc.type | article | en_US |
dc.contributor.department | RTEÜ, Fen - Edebiyat Fakültesi, Kimya Bölümü | en_US |
dc.contributor.institutionauthor | Özil, Musa | |
dc.contributor.institutionauthor | Baltaş, Nimet | |
dc.identifier.doi | 10.1002/ardp.202200400 | en_US |
dc.relation.journal | Archiv der Pharmazie | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |