Author/Authors :
Nagao، نويسنده , , Yoshimitsu and Sano، نويسنده , , Shigeki and Morimoto، نويسنده , , Kenji and Kakegawa، نويسنده , , Hisao and Takatani، نويسنده , , Tadanobu and Shiro، نويسنده , , Motoo and Katunuma، نويسنده , , Nobuhiko، نويسنده ,
Abstract :
Chiral 5-substituted 3-pyrrolin-2-ones bearing l-Ile-l-Pro-OH or l-Phe-NHCH2Ph were successfully synthesized by utilizing a characteristic reaction cascade based on alkaline hydrolysis of the corresponding diethyl α-hydroxy-α-(β-propiolamide)malonates. Among the synthesized chiral pyrrolinones, compound 5S-9 proved to be the most potent inhibitor against cathepsin B.
Keywords :
enzyme inhibitor , Alkynes , cyclization , lactams , X-ray crystal structures
