Potent and selective thrombin inhibitors featuring hydrophobic, basic P-3-P-4-aminoalkyllactam moieties

Crystal structure and evolving SAR considerations of potent, selective benz ylsulfonamide lactam thrombin inhibitors and related serine protease inhibi tors have led to the design of novel thrombin inhibitors lag, featuring hyd rophobic, basic, P-4-alkylaminolactam scaffolds that serve as novel types o f P-3-P-4 dipeptide mimics. The design, synthesis, and biological activity of these targets is presented. (C) 1998 Elsevier Science Ltd. All rights re served.