Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus

Abstract The design and synthesis of a series of tripeptideacylsulfonamides as potent inhibitors of the HCV NS3/4A serine proteaseis described. These analogues house a C4 aryl, C4 hydroxy-proline at the S2 position of the tripeptidescaffold. Information relating to structure-activity relationshipsas well as the pharmacokinetic and cardiovascular profiles of these analogues is provided.