The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.
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.
D000818:Animals; D001682:Biological Availability; D006801:Humans; D007408:Intestinal Absorption; D051381:Rats; D017207:Rats, Sprague-Dawley; D013917:Thrombin / Q000008:administration & dosage* / Q000037:antagonists & inhibitors* / Q000493:pharmacokinetics