Synthesis of salicyl-peptides and their effect on human platelet aggregationin vitro

Autor:	A. Aaberg, Vassiliki Magafa, Georgios Stavropoulos, Maria Liakopoulou-Kyriakides, Z. Sinakos
Rok vydání:	1997
Předmět:	chemistry.chemical_classification Dipeptide Platelet aggregation Stereochemistry Organic Chemistry Clinical Biochemistry Human platelet Inhibitory postsynaptic potential Biochemistry In vitro Amino acid chemistry.chemical_compound chemistry Leucine IC50
Zdroj:	Amino Acids. 13:171-181
ISSN:	1438-2199 0939-4451
Popis:	A series of leucine dipeptide amides containing at their N-terminal amino group the salicyl-residue [(o)-RO-C6H4-CO-, where R=H or CH3CO] have been synthesized by conventional solution techniques and tested for their inhibitory activity on human platelet aggregationin vitro induced by collagen, ADP or adrenaline. The salicyl-peptide (o)-HO-C6H4-CO-Leu-Asp(OBzl)-NH2 was found to exert strong inhibitory activity on platelet aggregation induced by collagen with an IC50 value 4.5 mM. The corresponding dipetide H2N-Leu-Asp(OVzl)-NH2 was also examined and was found to be less active, indicating that the presence of the lipophilicβ-benzyl ester group in combination with the salicyl group enhance the inhibitory activity. All the other salicyl-peptides examined either didn't show any inhibitory or aggregatory activity or a slight inhibition at the concentration of 9–10 mm.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::33ffaea1a410776396b2404fd6c035cc https://doi.org/10.1007/bf01373215 Zobrazit plný text záznamu Full text from SpringerLink