Academic Journal
Design, synthesis, and evaluation of novel substituted imidazo[1,2-c]quinazoline derivatives as potential α-glucosidase inhibitors with bioactivity and molecular docking insights
| العنوان: | Design, synthesis, and evaluation of novel substituted imidazo[1,2-c]quinazoline derivatives as potential α-glucosidase inhibitors with bioactivity and molecular docking insights |
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| المؤلفون: | Fariba Peytam, Faezeh Sadat Hosseini, Reza Fathimolladehi, Mohammad Javad Dehghan Nayeri, Mahdis Sadeghi Moghadam, Bahareh Bayati, Maryam Norouzbahari, Roham Foroumadi, Fahimeh Bonyasi, Ruzbehan Divsalar, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Maliheh Barazandeh Tehrani, Loghman Firoozpour, Alireza Foroumadi |
| المصدر: | Scientific Reports, Vol 14, Iss 1, Pp 1-23 (2024) |
| بيانات النشر: | Nature Portfolio, 2024. |
| سنة النشر: | 2024 |
| المجموعة: | LCC:Medicine LCC:Science |
| مصطلحات موضوعية: | Diabetes, α-Glucosidase, Imidazo[1,2-c]quinazoline, Imidazoquinazoline, Medicine, Science |
| الوصف: | Abstract α-Glucosidase inhibitors are important in the treatment of type 2 diabetes by regulating blood glucose levels and reducing carbohydrate absorption. The present study focuses on identifying new inhibitors bearing imidazo[1,2-c]quinazoline backbone through multi-step synthesis. The inhibitory potencies of the novel derivatives were tested against Saccharomyces cerevisiae α-glucosidase, revealing IC50 values ranging from 50.0 ± 0.12 µM to 268.25 ± 0.09 µM. Among them, 2-(4-(((2,3-diphenylimidazo[1,2-c]quinazolin-5-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-(2-methoxyphenyl)acetamide (19e) and 2-(4-((benzo[4,5]imidazo[1,2-c]quinazolin-6-ylthio)methyl)-1H-1,2,3-triazol-1-yl)-N-(2-methoxyphenyl)acetamide (27e) emerged as the most potent inhibitors and were further investigated in various assessments. Finally, molecular docking studies were performed to reveal the crucial binding interactions and to confirm the results obtained from structure-activity relationship (SAR) analysis. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 2045-2322 |
| Relation: | https://doaj.org/toc/2045-2322 |
| DOI: | 10.1038/s41598-024-78878-2 |
| URL الوصول: | https://doaj.org/article/82b194149e1146c9a9bbc89d29a3ad76 |
| رقم الانضمام: | edsdoj.82b194149e1146c9a9bbc89d29a3ad76 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 20452322 |
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| DOI: | 10.1038/s41598-024-78878-2 |