Partially modified retro-inverso enkephalin analogues containing Gly 3 Ψ (NH-CO) Phe 4 modification, Configurational lability

…, E Ackerman, D Levian-Teitelbaum…

Index: Chorev, Michael; Gilon, Noemy; Roubini, Eli; Ackerman, Elizabeth; Levian-Teitelbaum, Dina; Rosin, Marta Collection of Czechoslovak Chemical Communications, 1988 , vol. 53, # 11A p. 2519 - 2536

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Citation Number: 6

Abstract

Abstract Two partially modified retro-inverso analogues of Leu-enkephalin in which the peptide bond between Gly 3-Phe 4 was reversed resulted from the incorporation of the Gly 3 ψ (NH-CO) Phe 4 unit. The presence of racemic 2-benzylmalonyl residue led to diastereomeric mixtures of analogues; H-Tyr-D-Ala-gGly-(RS)-mPhe-Leu-NH 2 (I) and H-Tyr- Gly-gGly-(RS)-mPhe-Leu-NH 2 (II). Analogue I was more potent than analogue II in the ...