dc.contributor.author | Saleem, Faiza | |
dc.contributor.author | Shamim, Fariha | |
dc.contributor.author | Özil, Musa | |
dc.contributor.author | Baltaş, Nimet | |
dc.contributor.author | Salar, Uzma | |
dc.contributor.author | Ashraf, Sajda | |
dc.contributor.author | Ul-Haq, Zaheer | |
dc.contributor.author | Taha, Muhammad | |
dc.contributor.author | Solangi, Mehwish | |
dc.contributor.author | Khan, Khalid Mohammed | |
dc.date.accessioned | 2023-10-24T05:45:53Z | |
dc.date.available | 2023-10-24T05:45:53Z | |
dc.date.issued | 2023 | en_US |
dc.identifier.citation | Saleem, F., Shamim, F., Özil, M., Baltaş, N., Salar, U., Ashraf, S., Ul-Haq, Z., Taha, M., Solangi, M., & Khan, K. M. (2023). Multicomponent diastereoselective synthesis of tetrahydropyridines as α-amylase and α-glucosidase enzymes inhibitors. Future medicinal chemistry, 15(15), 1343–1368. https://doi.org/10.4155/fmc-2023-0073 | en_US |
dc.identifier.issn | 1756-8919 | |
dc.identifier.issn | 1756-8927 | |
dc.identifier.issn | 1756-8919 | |
dc.identifier.uri | https://doi.org/10.4155/fmc-2023-0073 | |
dc.identifier.uri | https://hdl.handle.net/11436/8556 | |
dc.description.abstract | Background: Researchers seeking new drug candidates to treat diabetes mellitus have been exploring bioactive molecules found in nature, particularly tetrahydropyridines (THPs). Methods: A library of THPs (1–31) were synthesized via a one-pot multicomponent reaction and investigated for their inhibition potential against α-glucosidase and α-amylase enzymes. Results: A nitrophenyl-substituted compound 5 with IC50 values of 0.15 ± 0.01 and 1.10 ± 0.04 μM, and a Km value of 1.30 mg/ml was identified as the most significant α-glucosidase and α-amylase inhibitor, respectively. Kinetic studies revealed the competitive mode of inhibition, and docking studies revealed that compound 5 binds to the enzyme by establishing hydrophobic and hydrophilic interactions and a salt bridge interaction with His279. Conclusion: These molecules may be a potential drug candidate for diabetes in the future. | en_US |
dc.language.iso | eng | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | α-amylase activity | en_US |
dc.subject | α-glucosidase activity | en_US |
dc.subject | In silico | en_US |
dc.subject | In vitro | en_US |
dc.subject | Kinetic studies | en_US |
dc.subject | Pyridine | en_US |
dc.title | Multicomponent diastereoselective synthesis of tetrahydropyridines as α-amylase and α-glucosidase enzymes inhibitors | 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 | 10.4155/fmc-2023-0073 | en_US |
dc.identifier.volume | 15 | en_US |
dc.identifier.issue | 15 | en_US |
dc.identifier.startpage | 1343 | en_US |
dc.identifier.endpage | 1368 | en_US |
dc.relation.journal | Future Medicinal Chemistry | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |