Potent and selective bicyclic lactam inhibitors of thrombin: part 2: P1 modifications
…, JJ Edmunds, JX He, DR Holland, S Levesque…
文献索引：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
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.
