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.
Jang
Soyong
S
Department of Neuroscience and Medical Research Institute, School of Medicine, Ewha Womans University, Seoul 158-710, South Korea.
Jung
Jae-Chul
JC
Oh
Seikwan
S
D000818:Animals; D002599:Chalcone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D017628:Microglia / Q000187:drug effects; D009569:Nitric Oxide / Q000096:biosynthesis; D010084:Oxidation-Reduction; D013055:Spectrophotometry, Infrared
D009569:Nitric Oxide; D002599:Chalcone