Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities

Soyong Jang, Jae Chul Jung, Seikwan Oh

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16 Scopus citations

Abstract

A simple synthesis and biological properties of 1,3-diphenyl-2-propen-1-ones 18-22 and 25-26 are described. The key synthetic strategies involve Grignard reaction of aldehyde 2 and oxidation reaction of 8-12 in high yields. The prepared compounds 18-22 and 25-26 were evaluated for free-radical scavenging, suppression of LPS-induced NO generation, and anti-excitotoxicity in vitro. It was found that a couple of compounds, especially 21 and 26, were potent suppressors of NO generation and demonstrated anti-excitotoxicity with the concentration range 10-20 μM in vitro.

Original languageEnglish
Pages (from-to)4098-4105
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume15
Issue number12
DOIs
StatePublished - 15 Jun 2007

Keywords

  • 1,3-Diphenyl-2-propen-1-ones
  • Anti-excitotoxicity
  • Grignard reaction
  • NO-generation

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