Physiologically active tetrapeptides

C - Chemistry – Metallurgy – 07 – C

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530/5.1

C07C 103/52 (1980.01)

Patent

CA 1182110

PHYSIOLOGICALLY ACTIVE TETRAPEPTIDES ABSTRACT This invention provides tetrapeptide derivatives of the formula (I): Image (I) wherein R1 and R2 are methyl, 1-methylethyl, 2-methylpropyl, 1-hydroxyethyl, 2-carboxyethyl or 4-aminobutyl and Y is Image wherein R3 is methyl, 1-methylethyl, 2-methylpropyl, 1-methylpropyl, hydroxymethyl, 1-hydroxyethyl, carboxy- methyl, 2-carboxyethyl, 4-aminobutyl, 3-guanidinopropyl, benzyl or p-hydroxybenzyl excluding the compounds in which R1 and R2 are each 1-methylethyl and also R3 is carboxymethyl or 2-carboxyethyl, the first and leftmost .beta.-amino acid moiety in said tetrapeptide derivatives having the (2S,3R)- configuration and a primary amino group and the second, third and fourth .alpha.-amino acid moieties in said tetrapeptide derivatives having the L-configuration. These compounds have an inhibitory activity on several types of amino- peptidases.

355887

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