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Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications |
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| Authors: | JS Plummer KA Berryman C Cai WL Cody J DiMaio AM Doherty JJ Edmunds JX He DR Holland S Levesque DR Kent LS Narasimhan JR Rubin ST Rapundalo MA Siddiqui AJ Susser Y St-Denis PD Winocour |
| Affiliation: | Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA. |
| 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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