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 ...
[Kim, Sangsoo; Hwang, Sang Yeul; Kim, Young Kwan; Yun, Mikyung; Oh, Yeong Soo Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 7 p. 769 - 774]
