This review article illustrates the growing use of azaindole derivatives as kinase inhibitors and their contribution to drug discovery and innovation. The different protein kinases which have served as targets and the known molecules which have emerged from medicinal chemistry and Fragment-Based Drug Discovery (FBDD) programs are presented. The various synthetic routes used to access these compounds and the chemical pathways leading to their synthesis are also discussed. An analysis of their mode of binding based on X-ray crystallography data gives structural insights for the design of more potent and selective inhibitors.
23 December 2005 in Journal of Medicinal Chemistry
New membranes based on chitosan and chitosan-hyaluronic acid containing new arginine derivatives with thiazolidine-4-one scaffold have been prepared using the ionic cross-linking method. The presence of the arginine derivatives with thiazolidine-4-one scaffold into the polymer matrix was proved by Fourier-transform infrared spectroscopy (FT-IR). The scanning electron microscopy (SEM) revealed a micro-porous structure that is an important characteristic for the treatment of burns, favoring the exudate absorption, the rate of colonization, the cell structure, and the angiogenesis process. The developed polymeric membranes also showed good swelling degree, improved hydrophilicity, and biocompatibility in terms of surface free energy components, which supports their application for tissue regeneration. Moreover, the chitosan-arginine derivatives (CS-6h, CS-6i) and chitosan-hyaluronic acid-arginine derivative (CS-HA-6h) membranes showed good healing effects on the burn wound model induced to rats. For these membranes a complete reepithelialization was observed after 15 days of the experiment, which supports a faster healing process.