ChemInform Abstract: New Pepstatin Analogues: Synthesis and Pepsin Inhibition.

Abstract

New Pepstatin Analogues: Synthesis and Pepsin Inhibition.-Eight diastereomeric tripeptide analogues (VI) and (VII) are prepared from the protected amino acid methyl esters (I) via reduction, coupling with ethyl acetate (III), separation of the diastereomeric hydroxy esters (IV) by high performance liquid chromatography, deprotection, condensation with the mixed anhydride of (V), and final saponification. The analogues are less active than pepstatin as inhibitors of the pepsin hydrolysis of hemoglobin. -(MCCONNELL, R. M.; FRIZZELL, D.; CAMP, A.; EVANS, A.; JONES, W.; CAGLE, C.; J. Med.