Diphenyl-substituted triazine derivatives : synthesis, α-glucosidase inhibitory activity, kinetics and in silico studies
Background: Diabetes mellitus (DM) is a chronic disorder, considered to be a major global health challenge in the 21st century. α-Glucosidase enzyme is a well-known drug target to treat Type II DM. Methods: A new library of biphenyl-substituted triazines was synthesized and confirmed by various spectroscopic techniques. Results: All compounds showed potent α-glucosidase inhibitory activity, with IC50 values ranging from 35.35 ± 0.34 to 564.41 ± 0.91 μM, as the standard acarbose, IC50 value of 750.7 ± 0.13 μM. Our in silico study has predicted key interactions with the enzyme's active site. Drug-likeness and absorption, distribution, metabolism, excretion and toxicity were also studied. Conclusion: This study has identified a range of potential hits against the α-glucosidase enzyme that may serve as antidiabetic agents after further investigations.
| 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), 18 vom: 14. Sept., Seite 1651-1668 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Shamim, Shahbaz [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 23.10.2023 Date Revised 24.10.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0057 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM362247943 |
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| 245 | 1 | 0 | |a Diphenyl-substituted triazine derivatives |b synthesis, α-glucosidase inhibitory activity, kinetics and in silico studies |
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| 500 | |a Date Revised 24.10.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Background: Diabetes mellitus (DM) is a chronic disorder, considered to be a major global health challenge in the 21st century. α-Glucosidase enzyme is a well-known drug target to treat Type II DM. Methods: A new library of biphenyl-substituted triazines was synthesized and confirmed by various spectroscopic techniques. Results: All compounds showed potent α-glucosidase inhibitory activity, with IC50 values ranging from 35.35 ± 0.34 to 564.41 ± 0.91 μM, as the standard acarbose, IC50 value of 750.7 ± 0.13 μM. Our in silico study has predicted key interactions with the enzyme's active site. Drug-likeness and absorption, distribution, metabolism, excretion and toxicity were also studied. Conclusion: This study has identified a range of potential hits against the α-glucosidase enzyme that may serve as antidiabetic agents after further investigations | ||
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| 700 | 1 | |a Khan, Khalid Mohammed |e verfasserin |4 aut | |
| 700 | 1 | |a Ali, Muhammad |e verfasserin |4 aut | |
| 700 | 1 | |a Mahdavi, Mohammad |e verfasserin |4 aut | |
| 700 | 1 | |a Salar, Uzma |e verfasserin |4 aut | |
| 700 | 1 | |a Mohammadi-Khanaposhtani, Maryam |e verfasserin |4 aut | |
| 700 | 1 | |a Faramarzi, Mohammad Ali |e verfasserin |4 aut | |
| 700 | 1 | |a Ullah, Nisar |e verfasserin |4 aut | |
| 700 | 1 | |a Taha, Muhammad |e verfasserin |4 aut | |
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