Phenylamide inhibitors

Figure 1 N-carboxylalkyl inhibitor of sfSTR, N-[(R)-carboxyl-ethyl]-(S)-(2-phenylethyl) glycyl-L-arginine-N-phenylamide [8]. The convention of Schechter and Berger [61 ] is used to describe the specificity subsites of the enzyme Si, S2, S3 which correspond to the side chains P/, P2, P3 of the inhibitor. (From Ref. 5.)... 

From the industrial sector, in 2005, Cezanne et al. filed a patent on the synthesis of inhibitors of the coagulation factors XA and/or VIIA for treating thromboses [83]. The ligand-free Cu(I)-catalyzed amidation of aryl bromides with lactams was employed as the key step leading to 2-(phenyl)-2W-pyrazole-3-carboxylic acid-A/-4-(thioxo-heterocyclyl)phenylamide derivatives and the corresponding imino-heterocyclyl derivatives. 

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