Sherafati, M. and Mirzazadeh, R. and Barzegari, E. and Mohammadi-Khanaposhtani, M. and Azizian, H. and Sadegh Asgari, M. and Hosseini, S. and Zabihi, E. and Mojtabavi, S. and Ali Faramarzi, M. and Mahdavi, M. and Larijani, B. and Rastegar, H. and Hamedifar, H. and Hamed Hajimiri, M. (2021) Quinazolinone-dihydropyrano3,2-bpyran hybrids as new α-glucosidase inhibitors: Design, synthesis, enzymatic inhibition, docking study and prediction of pharmacokinetic. Bioorganic Chemistry, 109.
Full text not available from this repository.Abstract
A series of new quinazolinone-dihydropyrano3,2-bpyran derivatives 10A-L were synthesized by simple chemical reactions and were investigated for inhibitory activities against α-glucosidase and α-amylase. New synthesized compounds showed high α-glucosidase inhibition effects in comparison to the standard drug acarbose and were inactive against α-amylase. Among them, the most potent compound was compound 10L (IC50 value = 40.1 ± 0.6 µM) with inhibitory activity around 18.75-fold more than acarboase (IC50 value = 750.0 ± 12.5 µM). This compound was a competitive inhibitor into α-glucosidase. Our obtained experimental results were confirmed by docking studies. Furthermore, the cytotoxicity of the most potent compounds 10L, 10G, and 10N against normal fibroblast cells and in silico druglikeness, ADME, and toxicity prediction of these compounds were also evaluated. © 2021 Elsevier Inc.
| Item Type: | Article |
|---|---|
| Additional Information: | cited By 0 |
| Subjects: | QV Pharmacology |
| Depositing User: | eprints admin |
| Date Deposited: | 29 Oct 2022 10:02 |
| Last Modified: | 29 Oct 2022 10:02 |
| URI: | http://eprints.iums.ac.ir/id/eprint/39600 |
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