1021707-57-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 131980-30-8 (S)-2-((tert-butoxycarbonyl)amino)-3-(3-cyanophenyl)propanoic acid 
• 64-19-7 acetic acid 

Downstream Products

• 1021707-59-4 Boc-Phe(3-Tfa-Ame)-OH 
• 1354577-82-4 C₂HF₃O₂*C₄₅H₄₇N₇O₆S 
• 1354578-32-7 Boc-Phe(3-AMe-Cbz)-OMe 
• 1354578-34-9 C₂HF₃O₂*C₁₉H₂₂N₂O₄ 
• 1354578-35-0 C₄₄H₄₆N₄O₉S 
• 1357451-57-0 C₃₈H₄₀N₄O₇S 
• 1357451-59-2 C₃₇H₃₈N₄O₇S 
• 1354577-84-6 C₂HF₃O₂*C₄₅H₄₇N₇O₆S 
• 1354578-38-3 C₃₈H₄₀N₄O₇S 
• 1354578-39-4 C₃₇H₃₈N₄O₇S 
• 1354578-28-1 Boc-Phe(3-AMe-Cbz)-OH 

Relevant academic research and scientific papers

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

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 Ki of 0.77 and 2.4 nM, respectively, whereas it has poor activity against the related trypsin-like serine proteases thrombin, factor Xa, or activated protein C. Modeling experiments revealed that inhibitor 10 adopts a compact and rigid structure that fits well into the relatively open active site of plasmin and plasma kallikrein, while it is rejected from sterically demanding residues present in loops of the other enzymes. These results from modeling confirm the selectivity profile found for inhibitor 10 in enzyme kinetic studies. Such compounds might be useful lead structures for the development of new antifibrinolytic drugs for use in cardiac surgery with cardiopulmonary bypass or organ transplantations to reduce bleeding complications.

SERINE PROTEASE INHIBITORS

The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.

TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE

The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.