Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 quaternary lactam dipeptide surrogates

Article abstract of DOI:10.1016/S0960-894X(97)00446-0

SAR and molecular modeling investigations on the potent and selective thrombin inhibitor 1b (CVS 1578) and related serine protease inhibitors led to the design of series 2a-g, featuring quaternary α-amino-α-benzyl-lactam scaffolds that serve as novel P₃-P₄ dipeptide mimics. The design, synthesis, and biological activity of these targets an presented.