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PHYSIOLOGICALLY ACTIVE TETRAPEPTIDES

机译:生理活性四肽

摘要

PHYSIOLOGICALLY ACTIVE TETRAPEPTIDESABSTRACTThis invention provides tetrapeptide derivativesof the formula (I):(I)wherein R1 and R2 are methyl, 1-methylethyl, 2-methylpropyl,1-hydroxyethyl, 2-carboxyethyl or 4-aminobutyl and Y iswherein 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 R1and R2 are each 1-methylethyl and also R3 is carboxymethylor 2-carboxyethyl, the first and leftmost .beta.-amino acidmoiety 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 tetrapeptidederivatives having the L-configuration. These compoundshave an inhibitory activity on several types of amino-peptidases.
机译:生理活性四肽抽象本发明提供了四肽衍生物式(I)的式子:(一世)其中R1和R2是甲基,1-甲基乙基,2-甲基丙基,1-羟乙基,2-羧乙基或4-氨基丁基,且Y为其中R3是甲基,1-甲基乙基,2-甲基丙基,1-甲基丙基,羟甲基,1-羟乙基,羧基甲基,2-羧乙基,4-氨基丁基,3-胍基丙基,苄基或对羟基苄基,但不包括其中R1的化合物和R2分别是1-甲基乙基,并且R3是羧甲基或2-羧乙基,第一个和最左边的β-氨基酸所述具有(2S,3R)-的四肽衍生物中的部分构型和伯氨基,第二个所述四肽中的第三和第四α-氨基酸部分具有L-构型的衍生物。这些化合物对几种类型的氨基肽酶。

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