Design and synthesis of novel pyridazine N-aryl acetamides : In-vitro evaluation of α-glucosidase inhibition, docking, and kinetic studies
Copyright © 2020 Elsevier Inc. All rights reserved..
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:102 |
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| Enthalten in: |
Bioorganic chemistry - 102(2020) vom: 15. Sept., Seite 104071 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Moghimi, Setareh [VerfasserIn] |
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| Links: |
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| Themen: |
Acetamides |
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| Anmerkungen: |
Date Completed 18.03.2021 Date Revised 18.03.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bioorg.2020.104071 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM312644302 |
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| 500 | |a Date Revised 18.03.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2020 Elsevier Inc. All rights reserved. | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Antidiabetic drug | |
| 650 | 4 | |a Glucosidase inhibitor | |
| 650 | 4 | |a Lawesson’s reagent | |
| 650 | 4 | |a Pyridazine | |
| 650 | 7 | |a Acetamides |2 NLM | |
| 650 | 7 | |a Glycoside Hydrolase Inhibitors |2 NLM | |
| 650 | 7 | |a alpha-Glucosidases |2 NLM | |
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| 700 | 1 | |a Toolabi, Mahsa |e verfasserin |4 aut | |
| 700 | 1 | |a Salarinejad, Somayeh |e verfasserin |4 aut | |
| 700 | 1 | |a Firoozpour, Loghman |e verfasserin |4 aut | |
| 700 | 1 | |a Sadat Ebrahimi, Seyed Esmaeil |e verfasserin |4 aut | |
| 700 | 1 | |a Safari, Fatemeh |e verfasserin |4 aut | |
| 700 | 1 | |a Mojtabavi, Somayeh |e verfasserin |4 aut | |
| 700 | 1 | |a Faramarzi, Mohammad Ali |e verfasserin |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
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