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Research Journal of Pharmacy and Technology
Year : 2019, Volume : 12, Issue : 3
First page : ( 1145) Last page : ( 1154)
Print ISSN : 0974-3618. Online ISSN : 0974-360X.
Article DOI : 10.5958/0974-360X.2019.00189.6

Synthesis of some novel barbital derivatives based on Carbohydrate as α-glucosidase inhibitors

Radhi Ali Jabbar1,*, Zimam Ezzat H.2, Al-Mulla Emad Abbas Jaffar3

1Faculty of Pharmacy, Al-Kafeel University, Najaf, Iraq

2Department of Chemistry, Faculty of Science, Kufa University, Najaf, Iraq

3Babylon Technical Institute, Al-Furat Al-Awsat Technical University, 54003, Al-Kuf, Iraq

*Corresponding Author E-mail: alijebar56@gmail.com

Online published on 18 May, 2019.

Abstract

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 αglucosidase 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.

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Keywords

Barbital, 1, 2, 3-triazole, teterazole, antibacterial activity and α-Glucosidase Inhibitors.

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