| Literature DB >> 27454620 |
Assem Barakat1, Mohammad Shahidul Islam2, Abdullah Mohammed Al-Majid2, Hazem A Ghabbour3, Sammer Yousuf4, Mahwish Ashraf4, Nimra Naveed Shaikh4, M Iqbal Choudhary5, Ruqaiya Khalil6, Zaheer Ul-Haq6.
Abstract
This paper describes a facile protocol, efficient, and environmentally benign for the synthesis a series of barbiturate acid substituted at C5 position 3a-o. The desired compounds subjected in vitro for different set of bioassays including against anti-oxidant (DPPH and super oxide scavenger assays), anti-cancer, α-glucosidase and β-glucuronidase inhibitions. Compound 3m (IC50=22.9±0.5μM) found to be potent α-glucosidase enzyme inhibitors and showed more activity than standard acarbose (IC50=841±1.73μM). Compound 3f (IC50=86.9±4.33μM) found to be moderate β-Glucuronidase enzyme inhibitors and showed activity comparatively less than the standard d-saccharic acid 1,4-lactone (IC50=45.75±2.16μM). Furthermore, in sillico investigation was carried out to investigate bonding mode of barbiturate acid derivatives.Entities:
Keywords: Anti-cancer; Anti-oxidant; Pyrimidine-2,4,6-trione; α-Glucosidase inhibitor; β-Glucuronidase inhibitor
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Year: 2016 PMID: 27454620 DOI: 10.1016/j.bioorg.2016.07.009
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275