Katsuhiko Iseki

Structure–activity relationship of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone)

Abstract This paper describes the discovery of a novel free radical scavenger, 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone, 1), as a potent antioxidant agent against lipid peroxidation. The structure-activity relationship of edaravone indicated that lipophilic substituents were essential to show its lipid peroxidation-inhibitory activity. In vivo studies revealed that edaravone showed brain-protective activity in a transient ischemia model.

A convenient synthesis of β-alkynylpropionic acids from β-propiolactones. Synthesis of 4,4,5,5-tetradehydro-9(O)-methano-Δ6(9α)-PGI1

A new prostacyclin analog, 4,4,5,5-tetradehydro-9(0)-methano-gD6(9α)-PGI, has been synthesized by utilizing the regiocontrolled cleavage of the β-propiolactone uith the dialkylaluminum acetylide.