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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 |
Authors: | Ventosa-Andrés, Pilar ![]() ![]() ![]() ![]() |
Keywords: | α-Amino nitriles Peptide-derived thioureas Peptide-derived ureas PAR1 antagonists Platelet antiaggregant activity |
Issue Date: | 2012 |
Publisher: | Elsevier |
Citation: | European Journal of Medicinal Chemistry 58: 98-111 (2012) |
Abstract: | By 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. |
URI: | http://hdl.handle.net/10261/112587 |
DOI: | 10.1016/j.ejmech.2012.10.015 |
Identifiers: | doi: 10.1016/j.ejmech.2012.10.015 issn: 0223-5234 e-issn: 1768-3254 |
Appears in Collections: | (IQM) Artículos |
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