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Benzoflavone derivatives as potent antihyperuricemic agents

Abstract

Two series of benzoflavone derivatives were rationally designed, synthesized and evaluated for their xanthine oxidase (XO) inhibitory potential. Among both the 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 the 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 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 hyperuricemic mice model when tested in vivo.

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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
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Benzoflavone derivatives as potent antihyperuricemic agents

    H. Singh, J. V. Singh, G. Mal, G. Kaur, M. K. Gupta, A. P. Singh, K. Nepali, S. Sharma and P. M. Singh Bedi, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00512E

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