Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-monocyclic arginine surrogates

Article abstract of DOI:10.1016/S0960-894X(02)00129-4

Investigations on P₂-P₃-heterocyclic dipeptide surrogates directed towards identification of an orally bioavailable thrombin inhibitor led us to pursue novel classes of achiral, non-covalent P₁-arginine derivatives. The design, synthesis, and biological activity of inhibitors NC1-NC30 that feature three classes of monocyclic P₁-arginine surrogates will be disclosed: (1) (hetero)aromatic amidines, amines and hydroxyamidines, (2) 2-aminopyrazines, and (3) 2-aminopyrimidines and 2-aminotetrahydropyrimidines.