40524-65-0

Upstream product

• 888-12-0 (E)-2'-hydroxy-chalcone 
• 100-39-0 benzyl bromide 
• 6948-61-4 (E)-1-(2-methoxyphenyl)-3-phenylprop-2-en-1-one 
• 100-52-7 benzaldehyde 
• 579-74-8 2-Methoxyacetophenone 
• 31165-67-0 2'-benzyloxyacetophenone 

Relevant academic research and scientific papers

SYNUCLEINOPATHY THERAPEUTIC MEDICATION

This invention provides a pharmaceutical composition for treating or preventing synucleinopathy comprising a compound represented by formula (I), or a pharmaceutically acceptable salt thereof.

Practical synthesis of lespedezol A1

A practical formal synthesis of lespedezol A1 (1) was accomplished in 33% yield for four steps starting from formation of the substituted chalcone. Of particular note is a useful protocol for reduction of the 2-ene bond in the isoflavone intermediate. A significant improvement in the final ring closure when water was scavenged from the reaction is also noteworthy. The ready availability of lespedezol A1 will provide material for further pharmacological evaluation and for exploration of the pterocarpene nucleus as a potential entry into various 6a-hydroxypterocarpans.

2'-Substituted chalcone derivatives as inhibitors of interleukin-1 biosynthesis

A series of 2'-substituted chalcone derivatives has been found to show potent inhibition of the production of IL-1β from human peripheral blood monocytes stimulated with lipopolysaccharide (LPS), with IC50 values in the 0.2-5.0-μM range. Some members of the series have also shown inhibition of septic shock induced in mice by injection of LPS, although with low potency. Qualitative structure-activity relationships have shown that the enone is required for activity, which may be mediated by conjugate addition of a biological nucleophile to the chalcone. Electron-poor aromatic rings β to the ketone give enhanced potency. Although electronic effects in the other ring (directly attached to the ketone) are minimal, this ring must possess an ortho substituent for good activity without cytotoxicity, suggesting a degree of selectivity which would not be expected for simple, nonspecific alkylating agents.