Hinkes, Stefan; Wuttke, Andre; Saupe, Sebastian M.; Ivanova, Teodora; Wagner, Sebastian; Knoerlein, Anna; Heine, Andreas; Klebe, Gerhard; Steinmetzer, Torsten published an article in Journal of Medicinal Chemistry. The title of the article was 《Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines》.Product Details of 67877-95-6 The author mentioned the following in the article:
New macrocyclic plasmin inhibitors based on our previously optimized P2-P3 core segment have been developed. In the first series, the P4 residue was modified, whereas the 4-amidinobenzylamide in P1 position was maintained. The originally used P4 benzylsulfonyl residue could be replaced by various sulfonyl- or urethane-like protecting groups. In the second series, the P1 benzamidine was modified and a strong potency and excellent selectivity was retained by incorporation of p-xylenediamine. Several analogs inhibit plasmin in the subnanomolar range, and their potency against related trypsin-like serine proteases including trypsin itself could be further reduced. Selected derivatives have been tested in a plasma fibrinolysis assay and are more effective than the reference inhibitor aprotinin. The crystal structure of one inhibitor was determined in complex with trypsin. The binding mode reveals a sterical clash of the inhibitor’s linker segment with the 99-hairpin loop of trypsin, which is absent in plasmin. In the experiment, the researchers used H-D-Phe(4-NO2)-OMe.HCl(cas: 67877-95-6Product Details of 67877-95-6)
H-D-Phe(4-NO2)-OMe.HCl(cas: 67877-95-6) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Product Details of 67877-95-6 Polyesters are important plastics, with monomers linked by ester moieties.
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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics