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

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

文献索引：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

全文：HTML全文

被引用次数: 10

摘要

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 ...