Potent and selective thrombin inhibitors featuring hydrophobic, basic P3-P4-aminoalkyllactam moieties

Article abstract of DOI:10.1016/S0960-894X(98)00636-2

Crystal structure and evolving SAR considerations of potent, selective benzylsulfonamide lactam thrombin inhibitors and related serine protease inhibitors have led to the design of novel thrombin inhibitors lag, featuring hydrophobic, basic, P₄-alkylaminolactam scaffolds that serve as novel types of P₃-P₄ dipeptide mimics. The design, synthesis, and biological activity of these targets is presented.