Synthesis and Structure-Activity Relationship of Potent Bicyclic Lactam Thrombin Inhibitors.

A simple and versatile method for preparation of (D)-Phe-Pro peptidomimetic bicyclic thiazolidine lactams is presented. These bicyclic lactams have chemical diversity α to the lactam carbonyl and, when linked to electrophilic arginines, provide potent thrombin inhibitors.