The discovery of orally available thrombin inhibitors: Optimisation of the P1 pharmacophore

Article abstract of DOI:10.1016/S0960-894X(99)00138-9

Thrombin inhibitors have been designed with the replacement of the strongly basic guanidine P1 pharmocophore with a group that exploits the lipophilicity of the S1 pocket. The approach has lead to the discovery of potent thrombin inhibitors demonstrating good intra-duodenal absorption.