59617-94-6Relevant academic research and scientific papers
Synthesis and activity of pyrrolidinyl- and thiazolidinyl-dipeptide derivatives as inhibitors of the Tc80 prolyl oligopeptidase from Trypanosoma cruzi
Joyeau, Roger,Maoulida, Chanfi,Guillet, Cindy,Frappier, Francois,Teixeira, Antonio R.L.,Schrevel, Joseph,Santana, Jaime,Grellier, Philippe
, p. 257 - 266 (2007/10/03)
Pyrrolidinyl- and thiazolidinyl- dipeptide derivatives, featuring either a vinyl sulfone-, a 2-ketobenzothiazole-, a nitrile-, or a benzimidazole group at the C-terminus, were designed and synthesized as potential inhibitors of the prolyl-specific Tc80 proteinase from Trypanosoma cruzi, the agent of Chagas' disease. These compounds were evaluated in vitro towards the target enzyme which was classified as a serine protease belonging to the prolyl oligopeptidase family (EC 3.4.21.26). A peptidyl nitrile and two peptidyl α-ketobenzothiazoles were shown to be potent reversible and competitive inhibitors of Tc 80 proteinase, with K(i) values in the range 38- 219 nM, and compared advantageously with some known mammalian prolyl oligopeptidase inhibitors. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
