Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: Further focus on the contracted C4′-side chain analogues

Abstract

Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4′-side chain series. SAR studies identified compounds with either a pyrrolidino or morpholino group as potent, active site directed thrombin inhibitors when the amino group was connected to the C3-phenyl ring with a methylene linker at the C4′ position of the phenyl ring.