Anti-glycemic potential of benzophenone thio/semicarbazone derivatives: synthesis, enzyme inhibition and ligand docking studies
| Autor: | Khalid Mohammed Khan, Sharmeen Fayyaz, Muniza Shaikh, Arshia, M. Iqbal Choudhary |
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| Rok vydání: | 2021 |
| Předmět: |
Blood Glucose
Semicarbazones Dipeptidyl-Peptidase IV Inhibitors animal structures endocrine system diseases Stereochemistry nutritional and metabolic diseases Thio Type 2 Diabetes Mellitus General Medicine Ligands Ligand (biochemistry) Molecular Docking Simulation Benzophenones chemistry.chemical_compound Enzyme inhibition Docking (dog) Diabetes Mellitus Type 2 chemistry Structural Biology Benzophenone Humans Molecular Biology Semicarbazone Glycemic |
| Zdroj: | Journal of Biomolecular Structure and Dynamics. 40:7339-7350 |
| ISSN: | 1538-0254 0739-1102 |
| DOI: | 10.1080/07391102.2021.1897045 |
| Popis: | Inhibition of dipeptidyl peptidase-IV (DPP-IV) has been identified as a promising approach for the treatment of type 2 diabetes mellitus (T2DM). Therefore, development of DPP-IV inhibitors with new chemical scaffold is of utmost importance to medicinal chemistry. In the present study, we identified benzophenone thio- and semicarbazone scaffolds as novel DPP-IV inhibitors. For that purpose, benzophenone thio- and semicarbazone were synthesized through a 2-step reaction. These newly synthetic derivatives were characterized by different spectroscopic techniques, including HREI-MS and NMR. whereas stereochemistry of the iminic bond was predicted by NOESY experiments. Thio- and semicarbazones derivatives were evaluated for their DPP-IV inhibitory potential and found to exhibit a good to moderate enzyme inhibitory activity. Most active and non-cytotoxic derivatives were further evaluated for their DPP-IV inhibitory potential in |
| Databáze: | OpenAIRE |
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