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 ...