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Issue 1, 2019
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Benzoflavone derivatives as potent antihyperuricemic agents

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Two series of benzoflavone derivatives were rationally designed, synthesized and evaluated for their xanthine oxidase (XO) inhibitory potential. Among both series, eight compounds (NF-2, NF-4, NF-9, NF-12, NF-16, NF-25, NF-28, and NF-32) were found to exert significant XO inhibition with IC50 values lower than 10 μM. Enzyme kinetic studies revealed that the most potent benzoflavone derivatives (NF-4 and NF-28) are mixed type inhibitors of the XO enzyme. Molecular modeling studies were also performed to investigate the binding interactions of these molecules (NF-4 and NF-28) with the amino acid residues present in the active site of the enzyme. Docking results confirmed that their favorable binding conformations in the active site of XO can completely block the catalytic activity of the enzyme. Benzoflavone derivatives exhibiting potent XO enzyme inhibition also showed promising results in a hyperuricemic mice model when tested in vivo.

Graphical abstract: Benzoflavone derivatives as potent antihyperuricemic agents

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Publication details

The article was received on 10 Oct 2018, accepted on 05 Dec 2018 and first published on 06 Dec 2018

Article type: Research Article
DOI: 10.1039/C8MD00512E
Med. Chem. Commun., 2019,10, 128-147

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    Benzoflavone derivatives as potent antihyperuricemic agents

    J. V. Singh, G. Mal, G. Kaur, M. K. Gupta, A. Singh, K. Nepali, H. Singh, S. Sharma and P. M. S. Bedi, Med. Chem. Commun., 2019, 10, 128
    DOI: 10.1039/C8MD00512E

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