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Triazoloquinazolines as a new class of potent ?-glucosidase inhibitors: in vitro evaluation and docking study.

ABSTRACT: 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 ?-glucosidase inhibitors using ?-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 ?M, respectively) in relation to that of acarbose (IC50 = 143.54 ± 2.08 ?M) as a reference drug. Triazoloquinazolines were identified herein as a new class of potent ?-glucosidase inhibitors. Molecular docking results envisaged the plausible binding interaction between the target triazoloquinazolines and ?-glucosidase enzyme and indicated considerable interaction with the active site residues.

SUBMITTER: Abuelizz HA

PROVIDER: S-EPMC6693780 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Triazoloquinazolines as a new class of potent α-glucosidase inhibitors: in vitro evaluation and docking study.

Abuelizz Hatem A HA Anouar El Hassane EH Ahmad Rohaya R Azman Nor Izzati Iwana Nor NIIN Marzouk Mohamed M Al-Salahi Rashad R

PloS one 20190814 8

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 α-glucosidase inhibitors using α-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 μM, respectively) in relation to that of acarbose (IC ...[more]

PMID: 31412050

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