Indole-pyridine carbonitriles : multicomponent reaction synthesis and bio-evaluation as potential hits against diabetes mellitus
Background: Diabetes mellitus is a significant health disorder; therefore, researchers should focus on discovering new drug candidates. Methods: A series of indole-pyridine carbonitrile derivatives, 1-34, were synthesized through a one-pot multicomponent reaction and evaluated for antidiabetic and antioxidant potential. Results: In this library, 12 derivatives - 1, 2, 4, 5, 7, 8, 10-12, 14, 15 and 31 - exhibited potent inhibitory activities against α-glucosidase and α-amylase enzymes, in comparison to acarbose (IC50 = 14.50 ± 0.11 μM). Furthermore, kinetics, absorption, distribution, metabolism, excretion and toxicity and molecular docking studies were used to interpret the type of inhibition, binding energies and interactions of ligands with target enzymes. Conclusion: These results indicate that the compounds may be promising hits for controlling diabetes mellitus and its related complications.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Future medicinal chemistry - 15(2023), 21 vom: 06. Nov., Seite 1943-1965 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Solangi, Mehwish [VerfasserIn] |
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| Links: |
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| Themen: |
ADME/Tox |
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| Anmerkungen: |
Date Completed 15.11.2023 Date Revised 22.11.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0087 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM364214147 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Background: Diabetes mellitus is a significant health disorder; therefore, researchers should focus on discovering new drug candidates. Methods: A series of indole-pyridine carbonitrile derivatives, 1-34, were synthesized through a one-pot multicomponent reaction and evaluated for antidiabetic and antioxidant potential. Results: In this library, 12 derivatives - 1, 2, 4, 5, 7, 8, 10-12, 14, 15 and 31 - exhibited potent inhibitory activities against α-glucosidase and α-amylase enzymes, in comparison to acarbose (IC50 = 14.50 ± 0.11 μM). Furthermore, kinetics, absorption, distribution, metabolism, excretion and toxicity and molecular docking studies were used to interpret the type of inhibition, binding energies and interactions of ligands with target enzymes. Conclusion: These results indicate that the compounds may be promising hits for controlling diabetes mellitus and its related complications | ||
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| 700 | 1 | |a Khan, Khalid Mohammed |e verfasserin |4 aut | |
| 700 | 1 | |a Ji, Xingyue |e verfasserin |4 aut | |
| 700 | 1 | |a Özil, Musa |e verfasserin |4 aut | |
| 700 | 1 | |a Baltaş, Nimet |e verfasserin |4 aut | |
| 700 | 1 | |a Salar, Uzma |e verfasserin |4 aut | |
| 700 | 1 | |a Khan, Alamgir |e verfasserin |4 aut | |
| 700 | 1 | |a Haq, Zaheer Ul |e verfasserin |4 aut | |
| 700 | 1 | |a Meghwar, Herchand |e verfasserin |4 aut | |
| 700 | 1 | |a Taha, Muhammad |e verfasserin |4 aut | |
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