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Synthesis of Some Novel Barbital Derivatives Based on Carbohydrate as α-Glucosidase Inhibitors
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A series of heterocyclic compounds were synthesized by reaction barbital derivatives with monosaccharaides derivatives. The structures of the prepared derivatives were identification by many spectroscopic methods including FTIR, 1H NMR, 13C NMR and Mass spectroscopy. The α-glucosidase inhibitory activities and antibacterial activities of some synthesized compounds were determination in vitro. All end compounds were showed α-glucosidase inhibitory activity in the range of (IC50 = 48.39 ±3.32–162.91±1.8μM) against the α-glucosidase enzyme when compared to the standard drug acarbose (IC50 = 787.27 ± 2.23 μM). Compounds 1t,2t,3t,4t and 5t showed significant α-glucosidase inhibitory activity with IC50 values of (162.91±1.8, 132.62±1.42, 68.44±2.11, 149.56±0.98, 48.39 ±3.32μM) respectively which were stronger than the positive controls acarbose. Compounds 5t and 3t have relatively higher therapeutic indices, representing potential promising leads. Overall result suggests that barbiturates with both five membered heterocyclic ring and monosaccharaides moiety could be lead a new design in the search of novel α-glucosidase inhibitor. Antibacterial activities of the synthesized compounds was screened against Escherichia coli and Staphylococcus aureus, using Azithromycin as reference.
Keywords
Barbital, 1,2,3-Triazole, Teterazole, Antibacterial Activity and α-Glucosidase Inhibitors.
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