Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety

Article abstract of DOI:10.1016/S0960-894X(98)00650-7

Replacement of the noragmatine group in thrombin inhibitors with a β- alanyl-guanidine group resulted in a nearly equipotent and more selective compound 8 despite the fact that the pK(a) of this P₁ moiety is five orders of magnitude lower. Furt