N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors

Kunal Nepali, Amit Agarwal, Sameer Sapra, Vineet Mittal, Raj Kumar, Uttam C. Banerjee, Manish K. Gupta, Naresh K. Satti, Om P. Suri, Kanaya L. Dhar

研究成果: 雜誌貢獻文章同行評審

47 引文 斯高帕斯(Scopus)

摘要

A series of forty two N-(1,3-diaryl-3-oxopropyl)amides were synthesized via an efficient, modified Dakin-West reaction and were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure-activity relationship analyses have been presented. Selected active xanthine oxidase inhibitors (3r, 3s, and 3zh) were assessed in vivo to study their anti-hyperuricemic effect in potassium oxonate induced hyperuricemic mice model. Compound 3s emerged as the most potent xanthine oxidase inhibitor (IC 50 = 2.45 μM) as well as the most potent anti-hyperuricemic agent. The basis of significant inhibition of xanthine oxidase by 3s was rationalized by its molecular docking into catalytic site of xanthine oxidase.
原文英語
頁(從 - 到)5569-5576
頁數8
期刊Bioorganic and Medicinal Chemistry
19
發行號18
DOIs
出版狀態已發佈 - 九月 15 2011
對外發佈Yes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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