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Synthesis of pyrimidine-2,4,6-trione derivatives: Anti-oxidant, anti-cancer, α-glucosidase, β-glucuronidase inhibition and their molecular docking studies.

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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Barakat A,Islam MS,Al-Majid AM,Ghabbour HA,Yousuf S,Ashraf M,Shaikh NN,Iqbal Choudhary M,Khalil R,Ul-Haq Z

doi

10.1016/j.bioorg.2016.07.009

subject

Has Abstract

pub_date

2016-10-01 00:00:00

pages

72-9

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(16)30132-8

journal_volume

68

pub_type

杂志文章

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