Potent and selective bicyclic lactam inhibitors of thrombin: part 2: P1 modifications

…, JJ Edmunds, JX He, DR Holland, S Levesque…

Index: Plummer, Janet S.; Berryman, Kent A.; Cai, Cuiman; Cody, Wayne L.; Dimaio, John; Doherty, Annette M.; Edmunds, Jeremy J.; He, John X.; Holland, Debra R.; Levesque, Sophie; Kent, Darin R.; Narasimhan, Lakshmi S.; Rubin, J. Ronald; Rapundalo, Stephen T.; Siddiqui, M. Arshad; Susser, Alan J.; St-Denis, Yves; Winocour, Peter D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 23 p. 3409 - 3414

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Citation Number: 29

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.