Synthesis and aldose reductase inhibitory activities of novel dibenzocycloheptenone derivatives

Jun Inoue, Ying She Cui, Libaniel Rodriguez, Zhou Chen, Peter F. Kador

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

A number of dibenzocycloheptenone derivatives, a novel series of aldose reductase inhibitors, were synthesized and evaluated in vitro for their ability to inhibit rat lens aldose reductase enzyme. The design of these ARIs was based on previously published pharmacophore requirements. The most active compound in this series was a spirosuccinimide derivative, spiro{2,8- dihydroxy-5H-dibenzo[a, d]cycloheptene5,3'-pyrrolidine}-2',5'-dione 11, having an IC50 of 3.0 μM.

Original languageEnglish (US)
Pages (from-to)399-404
Number of pages6
JournalEuropean Journal of Medicinal Chemistry
Volume34
Issue number5
DOIs
StatePublished - May 1999

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Keywords

  • Aldose reductase inhibitor
  • Diabetic complications
  • Dibenzocycloheptenone

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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