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Exploring the Phe-Gly Dipeptide-derived Piperazinone Scaffold in the search for Antagonists of the Thrombin receptor PAR1

AutorValdivielso, Ángel M.; García-López, M. Teresa ; Gutiérrez-Rodríguez, Marta ; Herranz, Rosario
Palabras claveEptidomimetics
Regioselectivity
Piperazinones platelet antiaggregant activity
PAR1 antagonists
Fecha de publicación2014
EditorMultidisciplinary Digital Publishing Institute
CitaciónMolecules 19: 4814-4846 (2014)
ResumenA series of Phe-Gly dipeptide-derived piperazinones containing an aromatic urea moiety and a basic amino acid has been synthesized and evaluated as inhibitors of human platelet aggregation induced by the PAR1 agonist SFLLRN and as cytotoxic agents in human cancer cells. The synthetic strategy involves coupling of a protected basic amino acid benzyl amide to 1,2- and 1,2,4-substituted-piperazinone derivatives, through a carbonylmethyl group at the N1-position, followed by formation of an aromatic urea at the exocyclic moiety linked at the C2 position of the piperazine ring and removal of protecting groups. None of the compounds showed activity in the biological evaluation. © 2014 by the authors; licensee MDPI, Basel, Switzerland.
URIhttp://hdl.handle.net/10261/97520
DOI10.3390/molecules19044814
Identificadoresdoi: 10.3390/molecules19044814
issn: 1420-3049
e-issn: 1420-3049
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