Exploring synthetic and therapeutic prospects of new thiazoline derivatives as aldose reductase (ALR2) inhibitors
This journal is © The Royal Society of Chemistry..
Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable approach for the development of new antidiabetic agents. With our ongoing interest towards aldose reductase (ALR2) inhibition, we have synthesized and screened a series of thiazoline derivatives (5a-k, 6a-f, 7a-1 & 8a-j) to find a lead as a potential new antidiabetic agent. The bioactivity results showed the thiazoline-based compound 7b having a benzyl substituent and nitrophenyl substituent-bearing compound 8e were identified as the most potent molecules with IC50 values of 1.39 ± 2.21 μM and 1.52 ± 0.78 μM respectively compared with the reference sorbinil with an IC50 value of 3.14 ± 0.02 μM. Compound 7b with only 23.4% inhibition for ALR1 showed excellent selectivity for the targeted ALR2 to act as a potential lead for the development of new therapeutic agents for diabetic complications.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
RSC advances - 11(2021), 28 vom: 06. Mai, Seite 17259-17282 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Shehzad, Muhammad Tariq [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Revised 30.04.2022 published: Electronic-eCollection Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1039/d1ra01716k |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM340086130 |
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| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a This journal is © The Royal Society of Chemistry. | ||
| 520 | |a Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable approach for the development of new antidiabetic agents. With our ongoing interest towards aldose reductase (ALR2) inhibition, we have synthesized and screened a series of thiazoline derivatives (5a-k, 6a-f, 7a-1 & 8a-j) to find a lead as a potential new antidiabetic agent. The bioactivity results showed the thiazoline-based compound 7b having a benzyl substituent and nitrophenyl substituent-bearing compound 8e were identified as the most potent molecules with IC50 values of 1.39 ± 2.21 μM and 1.52 ± 0.78 μM respectively compared with the reference sorbinil with an IC50 value of 3.14 ± 0.02 μM. Compound 7b with only 23.4% inhibition for ALR1 showed excellent selectivity for the targeted ALR2 to act as a potential lead for the development of new therapeutic agents for diabetic complications | ||
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| 700 | 1 | |a Imran, Aqeel |e verfasserin |4 aut | |
| 700 | 1 | |a Hameed, Abdul |e verfasserin |4 aut | |
| 700 | 1 | |a Rashida, Mariya Al |e verfasserin |4 aut | |
| 700 | 1 | |a Bibi, Marium |e verfasserin |4 aut | |
| 700 | 1 | |a Uroos, Maliha |e verfasserin |4 aut | |
| 700 | 1 | |a Asari, Asnuzilawati |e verfasserin |4 aut | |
| 700 | 1 | |a Iftikhar, Shafia |e verfasserin |4 aut | |
| 700 | 1 | |a Mohamad, Habsah |e verfasserin |4 aut | |
| 700 | 1 | |a Tahir, Muhammad Nawaz |e verfasserin |4 aut | |
| 700 | 1 | |a Shafiq, Zahid |e verfasserin |4 aut | |
| 700 | 1 | |a Iqbal, Jamshed |e verfasserin |4 aut | |
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