SUBSTRATE RELATED O,O-DIALKYLDIPEPTIDYLY ψ CARBOXYBENZYLPHOSPHONATES, A NEW TYPE OF THROMBIN INHIBITOR

Abstract O,O-Dialkyl α-hydroxybenzylphosphonates (1) were coupled to substrate derived dipeptides (2). using an active ester methodology approach to generate a series of phosphonotripeptides (3) with a carboxy ester linkage between the “P1” and “P2” positions of the molecule. These compounds inhibit thrombin in the micromolar range.