Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors

Article abstract of DOI:10.1016/S0960-894X(99)00130-4

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.