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Title

Design, synthesis and biological evaluation of new peptide-based ureas and thioureas as potential antagonists of the thrombin receptor PAR1

AuthorsVentosa-Andrés, Pilar ; Valdivielso, Ángel M. ; Pappos, Ioannis; García-López, M. Teresa ; Tsopanoglou, Nikos E.; Herranz, Rosario
Keywordsα-Amino nitriles
Peptide-derived thioureas
Peptide-derived ureas
PAR1 antagonists
Platelet antiaggregant activity
Issue Date2012
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 58: 98-111 (2012)
AbstractBy applying a diversity oriented synthesis strategy for the search of new antagonists of the thrombin receptor PAR1, a series of peptide-based ureas and thioureas, including analogues of the PAR1 reference antagonist RWJ-58259, has been designed and synthesized. The general synthetic scheme involves reduction of basic amino acid-derived amino nitriles by hydrogen transfer from hydrazine monohydrate in the presence of Raney Ni, followed by reaction with diverse isocyanates and isothiocyanates, and protecting group removal. All new compounds have been evaluated as inhibitors of human platelet aggregation induced by the PAR1 agonist SFLLRN. Some protected peptide-based ureas displayed significant antagonist activity.
URIhttp://hdl.handle.net/10261/112587
DOI10.1016/j.ejmech.2012.10.015
Identifiersdoi: 10.1016/j.ejmech.2012.10.015
issn: 0223-5234
e-issn: 1768-3254
Appears in Collections:(IQM) Artículos
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