Synthesis and pharmacological evaluation of peptide-mimetic protease-activated receptor-1 antagonists containing novel heterocyclic scaffolds

B Severino, F Fiorino, E Perissutti, F Frecentese…

Index: Severino, Beatrice; Fiorino, Ferdinando; Perissutti, Elisa; Frecentese, Francesco; Cirino, Giuseppe; Roviezzo, Fiorentina; Santagada, Vincenzo; Caliendo, Giuseppe Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 11 p. 6009 - 6020

Full Text: HTML

Citation Number: 10

Abstract

Protease-activated receptor-1 (PAR-1) is a G-coupled receptor activated by α-thrombin and other proteases. In this paper we describe the synthesis and the pharmacological evaluation of novel peptide-mimetic antagonists (compounds 1–16) characterized by the presence of new heterocyclic nuclei such as 2-methyl-indole (5-and 6-substituted) and 1, 4- benzodiazepine moiety. The new derivatives, tested in order to evaluate their antagonist ...

Related Articles:

Expedient Synthesis of 1-Hydroxy-4-and 1-Hydroxy-6-nitroindoles

[Bujok, Robert; Wrbel, Zbigniew; Wojciechowski, Krzysztof Synlett, 2012 , vol. 23, # 9 p. 1315 - 1320]

Synthesis of 4-and 6-substituted nitroindoles

[Moskalev, Nikolai; Barbasiewicz, Michal; Makosza, Mieczyslaw Tetrahedron, 2004 , vol. 60, # 2 p. 347 - 358]

Expedient Synthesis of 1-Hydroxy-4-and 1-Hydroxy-6-nitroindoles

[Bujok, Robert; Wrbel, Zbigniew; Wojciechowski, Krzysztof Synlett, 2012 , vol. 23, # 9 p. 1315 - 1320]

Expedient Synthesis of 1-Hydroxy-4-and 1-Hydroxy-6-nitroindoles

[Bujok, Robert; Wrbel, Zbigniew; Wojciechowski, Krzysztof Synlett, 2012 , vol. 23, # 9 p. 1315 - 1320]

More Articles...