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Molecules 2014, 19(4), 4814-4846; doi:10.3390/molecules19044814

Exploring the Phe-Gly Dipeptide-Derived Piperazinone Scaffold in the Search for Antagonists of the Thrombin Receptor PAR1

Instituto de Química Médica (CSIC), Juan de la Cierva 3, 28006 Madrid, Spain
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Received: 4 February 2014 / Revised: 8 April 2014 / Accepted: 13 April 2014 / Published: 16 April 2014
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Abstract

A 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. View Full-Text
Keywords: peptidomimetics; regioselectivity; piperazinones; platelet antiaggregant activity; PAR1 antagonists peptidomimetics; regioselectivity; piperazinones; platelet antiaggregant activity; PAR1 antagonists
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MDPI and ACS Style

Valdivielso, Á.M.; García-López, M.T.; Gutiérrez-Rodríguez, M.; Herranz, R. Exploring the Phe-Gly Dipeptide-Derived Piperazinone Scaffold in the Search for Antagonists of the Thrombin Receptor PAR1. Molecules 2014, 19, 4814-4846.

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