Screening of a library of 4-aryl/heteroaryl-4H-fused pyrans for xanthine oxidase inhibition: Synthesis, biological evaluation and docking studies

Ramandeep Kaur, Fatima Naaz, Sahil Sharma, Samir Mehndiratta, Manish Kumar Gupta, Preet Mohinder Singh Bedi, Kunal Nepali

研究成果: 雜誌貢獻文章同行評審

35 引文 斯高帕斯(Scopus)

摘要

A series of 4-aryl/heteroaryl-4H-fused pyrans was synthesized via multicomponent reaction in a microwave synthesizer. All the pyrans were evaluated for in vitro xanthine oxidase inhibition. Structure-activity relationship was also established. Among the series of 108 compounds, Compound 5n was the most potent displaying remarkable inhibition against the enzyme with an IC50 value of 0.59 μM. Enzyme kinetic study was carried out for the compound 5n to determine the type of inhibition. The study revealed that the compound 5n was a mixed-type inhibitor. Molecular modelling studies were also performed to figure out the interactions of both the enantiomers of 5n with the amino acid residues of the enzyme.
原文英語
頁(從 - 到)3334-3349
頁數16
期刊Medicinal Chemistry Research
24
發行號8
DOIs
出版狀態已發佈 - 八月 23 2015
對外發佈

ASJC Scopus subject areas

  • 藥理學、毒理學和藥劑學 (全部)
  • 有機化學

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