Triazoloquinazolines as a new class of potent alpha-glucosidase inhibitors: in vitro evaluation and docking study
Previously, we synthesized triazoloquinazolines 1-14 and characterized their structure. In this study, we aimed to evaluate the in vitro activity of the targets 1-14 as a-glucosidase inhibitors using a-glucosidase enzyme from Saccharomyces cerevisiae type 1. Among the tested compounds, triazoloquina...
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Format: | Article |
Language: | English |
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2019
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Online Access: | View Fulltext in Publisher |
LEADER | 01577nam a2200217Ia 4500 | ||
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001 | 10.1371-journal.pone.0220379 | ||
008 | 220223s2019 CNT 000 0 und d | ||
245 | 1 | 0 | |a Triazoloquinazolines as a new class of potent alpha-glucosidase inhibitors: in vitro evaluation and docking study |
260 | 0 | |c 2019 | |
650 | 0 | 4 | |a BIOLOGICAL EVALUATION |
650 | 0 | 4 | |a DERIVATIVES |
650 | 0 | 4 | |a MOLECULAR DOCKING |
856 | |z View Fulltext in Publisher |u https://doi.org/10.1371/journal.pone.0220379 | ||
520 | 3 | |a Previously, we synthesized triazoloquinazolines 1-14 and characterized their structure. In this study, we aimed to evaluate the in vitro activity of the targets 1-14 as a-glucosidase inhibitors using a-glucosidase enzyme from Saccharomyces cerevisiae type 1. Among the tested compounds, triazoloquinazolines 14, 8, 4, 5, and 3 showed the highest inhibitory activity (IC50 = 12.70 +/- 1.87, 28.54 +/- 1.22, 45.65 +/- 4.28, 72.28 +/- 4.67, and 83.87 +/- 5.12 mu M, respectively) in relation to that of acarbose (IC50 = 143.54 +/- 2.08 mu M) as a reference drug. Triazoloquinazolines were identified herein as a new class of potent a-glucosidase inhibitors. Molecular docking results envisaged the plausible binding interaction between the target triazoloquinazolines and alpha-glucosidase enzyme and indicated considerable interaction with the active site residues. | |
700 | 1 | 0 | |a Abuelizz, HA |e author |
700 | 1 | 0 | |a Ahmad, R |e author |
700 | 1 | 0 | |a Al-Salahi, R |e author |
700 | 1 | 0 | |a Anouar, E |e author |
700 | 1 | 0 | |a Azman, NIIN |e author |
700 | 1 | 0 | |a Marzouk, M |e author |
773 | |t PLOS ONE |