S-1 HETEROCYCLIC THROMBIN INHIBITORS

A series of boropeptides have previously been described by Kettner et al. to be potent thrombin inhibitors. DuP 714 is a representative of t his class of compounds with a K-i = 0.040 nM, but this inhibitor has u ndesireable side effects. New and selective boronic acid thrombin inhi bitors have been developed by replacing the guanidine of the boroargin ine side chain with various heterocycles ranging in size and basicity. Copyright (C) 1996 Elsevier Science Ltd