Aminopeptidase Inhibitory Properties and Analgesic Activity of (2 S ,3,7‐3,7‐Diamino‐2‐hydroxy‐heptanoic Acid Containing Tripeptide Analogues of the  N ‐Terminal Tripeptide of Probestin | Zendy

Herranz Rosario | Zendy; Vinuesa Soledad | Zendy; Pérez Concepción | Zendy; GarcíaLópez M. Teresa | Zendy; De Ceballos María L. | Zendy; Murillo Francisco M. | Zendy; Del Río Joaquín | Zendy

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Aminopeptidase Inhibitory Properties and Analgesic Activity of (2 S ,3,7‐3,7‐Diamino‐2‐hydroxy‐heptanoic Acid Containing Tripeptide Analogues of the N ‐Terminal Tripeptide of Probestin

Author(s) -

Herranz Rosario,

Vinuesa Soledad,

Pérez Concepción,

GarcíaLópez M. Teresa,

De Ceballos María L.,

Murillo Francisco M.,

Del Río Joaquín

Publication year - 1992

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.19923250812

Subject(s) - tripeptide , dipeptide , chemistry , stereochemistry , aminopeptidase , enkephalin , analgesic , peptide , inhibitory postsynaptic potential , enzyme inhibitor , in vitro , amino acid , biochemistry , opioid , pharmacology , leucine , receptor , medicine , neuroscience , biology

(2 S ,3 R )‐3,7‐Diamino‐2‐hydroxy‐heptanoyl‐Leu‐Pro‐OH [(2 S ,3 R )‐DAHHA‐Leu‐Pro‐OH, 4], analogue of the N ‐terminal tripeptide of probestin, has been synthesized, and tested as inhibitor of AP‐B, Leu‐AP, AP‐M, and enkephalin‐degrading APs, and as analgesic. In order to establish structure‐activity relationships the dipeptide (2 S ,3 R )‐DAHHA‐Pro‐OH ( 5 ) and the tripeptide (2 S , 3 R )‐DAHHA‐Ala‐Pro‐OH ( 6 ) were also prepared. Compounds 4 and 6 were potent and selective inhibitors of enkephalin‐degrading APs and showed a prolonged antinociceptive effect.

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