This invention provides tetrapeptide derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are methyl, 1- methylethyl, 2- methylpropyl, 1-hydroxyethyl, 2-carboxyethyl or 4- aminobutyl and Y is ##STR2## wherein R.sup.3 is methyl, 1-methylethyl, 2- methylpropyl, 1- methylpropyl, hydroxymethyl, 1-hydroxyethyl, carboxymethyl, 2- carboxyethyl, 4- aminobutyl, 3-guanidinopropyl, benzyl or p-hydroxybenzyl excluding the compounds in which R.sup.1 and R.sup.2 are each 1- methylethyl and also R.sup.3 is carboxymethyl or 2- carboxyethyl, the first and leftmost -amino acid moiety in said tetrapeptide derivatives having the (2S,3R)-configuration and a primary amino group and the second, third and fourth -amino acid moieties in said tetrapeptide derivatives having the L-configuration. These compounds have an inhibitory activity on several types of aminopeptidases.
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