Lawrence A. Vincent

Novel in vitro and in vivo inhibitors of prolyl endopeptidase

Abstract Inhibition of prolyl endopeptidase by Z-cyclohexyl prolinal and Z-indolinyl prolinal occurs with slow, tight binding inhibition and K i values of 2 – 3 nM. In vivo enzyme inhibition is also observed with a half time for recovery of enzyme activity of 3 – 4 h. Inhibition of prolyl endopeptidase by Z-cyclohexyl prolinal and Z-indolinyl prolinal occurs with slow, tight binding inhibition and K i values of 2 – 3 nM. In vivo enzyme inhibition is also observed with a half time for recovery of enzyme activity of 3 – 4 h.

Synthesis and stereochemistry of some thiazolidines related to 6-(hydroxyethyl)-penams.

Abstract L-Cysteine and D-penicillamine esters reacted with (R,R)- or (S,S)-2-t-butyl-5-dimethlylamino-methylene-6-methyl-[1,3]dioxan-4-one 3 to provide thiazolidines with high stereospecificity. The major products were potential precursors for cis-β-lactams.