A new strategy for the development of highly potent and selective plasmin inhibitors

SM Saupe, T Steinmetzer

Index: Saupe, Sebastian M.; Steinmetzer, Torsten Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1171 - 1180

Full Text: HTML

Citation Number: 20

Abstract

A new structure-based strategy for the design of potent and selective plasmin inhibitors was developed. These compounds could be prepared by cyclizations between the P3 and P2 amino acid residues of substrate-analogue inhibitors using metathesis or a copper- catalyzed azide alkyne cycloaddition in combination with standard peptide couplings. The most potent bis-triazole derivative 10 inhibits plasmin and plasma kallikrein with K i of 0.77 ...