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  • Title: Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.
    Author: Plummer JS, Berryman KA, Cai C, Cody WL, DiMaio J, Doherty AM, Edmunds JJ, He JX, Holland DR, Levesque S, Kent DR, Narasimhan LS, Rubin JR, Rapundalo ST, Siddiqui MA, Susser AJ, St-Denis Y, Winocour PD.
    Journal: Bioorg Med Chem Lett; 1998 Dec 01; 8(23):3409-14. PubMed ID: 9873743.
    Abstract:
    The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the P1 site. The introduction of arginine mimetics at the P1 site led to potent and selective thrombin inhibitors.
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