45158-94-9Relevant articles and documents
Polymeric hydrogels modified with ornithine and lysine: Sorption and release of metal cations and amino acids
Romanski, Jan,Karbarz, Marcin,Pyrzynska, Krystyna,Jurczak, Janusz,Stojek, Zbigniew
scheme or table, p. 542 - 550 (2012/04/23)
A novel, convenient synthesis, using copper ions, is described for the multigram-scale preparation of acryloyl and methacryloyl ornithine and lysine without the need to use protecting groups and chromatographic purifications. Three methods of removing the
Synthesis of pro-prodrugs l-lysine based for 5-aminosalicylic acid and 6-mercaptopurine colon specific release
Trombino, Sonia,Cassano, Roberta,Cilea, Alessia,Ferrarelli, Teresa,Muzzalupo, Rita,Picci, Nevio
experimental part, p. 290 - 296 (2012/06/29)
The aim of this work is to design, prepare and characterize l-lysine based prodrugs capable of targeting 6-mercaptopurine to the colon, an anti-tumor and immunosuppressant drug, and 5-aminosalicylic acid (5-ASA), drug of choice for inflammatory bowel disease (IBD). More specifically, Nε-feruloyl-S-(6- purinyl)-l-lysine and Nε-acryloyl-S-(6-purinyl)-l-lysine were synthesized and then characterized by FT-IR, 1H-NMR and GC/MS spectroscopies. The ability of feruloyl derivative in inhibiting lipid peroxidation in rat liver microsomal membranes, induced in vitro by tert-butyl hydroperoxide as source of free radicals, was evaluated. Moreover, Nε-acryloyl-S-(6-purinyl)-l-lysine, polymerizable prodrug, was used to microspheres realization for 5-ASA release. These lasts, obtained by emulsion inverse technique, were characterized by light scattering and scanning electron microscopy (SEM) analysis. The microspheres equilibrium swelling degree was evaluated and showed good swelling behaviour in simulating colonic fluids. Results confirm the possibility that the application range of l-lysine prodrug can be extended to the treatment of intestinal diseases whose conventional therapy envisages medications with serious side effects that, thanks to this new strategy, can be minimized in an optimal way.