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

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 microM in vitro.