Design and synthesis of novel pyridazine N-aryl acetamides: In-vitro evaluation of α-glucosidase inhibition, docking, and kinetic studies
| Autor: | Somayeh Mojtabavi, Loghman Firoozpour, Mohammad Ali Faramarzi, Mahsa Toolabi, Seyed Esmaeil Sadat Ebrahimi, Fatemeh Safari, Alireza Foroumadi, Setareh Moghimi, Somayeh Salarinejad |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Stereochemistry
Glucosidase Inhibitor 01 natural sciences Biochemistry Pyridazine Structure-Activity Relationship chemistry.chemical_compound Acetamides Drug Discovery medicine Humans Glycoside Hydrolase Inhibitors Cytotoxicity Molecular Biology Acarbose Molecular Structure 010405 organic chemistry Aryl Organic Chemistry alpha-Glucosidases In vitro 0104 chemical sciences Molecular Docking Simulation Kinetics 010404 medicinal & biomolecular chemistry chemistry Docking (molecular) Drug Design Lawesson's reagent medicine.drug |
| Zdroj: | Bioorganic Chemistry. 102:104071 |
| ISSN: | 0045-2068 |
| Popis: | We herein applied the four step-synthetic route to prepare the pyridazine core attached to the various N-aryl acetamides. By this approach, a new series of pyridazine-based compounds were synthesized, characterized and evaluated for their activities against α-glucosidase enzyme. In-vitro α-glucosidase assay established that twelve compounds are more potent than acarbose. Compound 7a inhibited α-glucosidase with the IC50 value of 70.1 µM. The most potent compounds showed no cytotoxicity against HDF cell line. Molecular docking and kinetic studies were performed to determine the modes of interaction and inhibition, respectively. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect