Hydroxyoxazolidines as α-aminoacetaldehyde equivalents: Novel inhibitors of calpain
4区 · 医学
Article
作者: Thaddeus R. Nieduzak ; Angela L. Marquart ; Julie N. White ; Philippe Bey ; Matthew D. Linnik ; Shujaath Mehdi ; Michael R. Angelastro ; Kin-Kai Hwang ; Dirk Friedrich ; Bart Emary ; Jack R. Koehl ; Hwa-Ok Kim ; Norton P. Peet ; Roy J. Vaz ; Mark E. Webster ; Gary A. Flynn
The synthesis of [1-[(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropy lcarbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described. Synthesis of related compounds, which offer insights into the mechanism of action for 2, are also described, as is an O-acetyl prodrug derivative of 2.