95215-87-5Relevant academic research and scientific papers
Investigation of the complexation ofnatZr(iv) and89Zr(iv) by hydroxypyridinones for the development of chelators for PET imaging applications
Guérard,Beyler,Lee,Tripier,Gestin,Brechbiel
, p. 4749 - 4758 (2017)
Three hydroxypyridinone (HOPO) positional isomers-1,2-HOPO (L1H) and its water soluble analogue (L1′H), 3,2-HOPO (L2H) and 3,4-HOPO (L3H) have been investigated for the complexation of Zr(iv). Potentiometric and
Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease
Lohou, Elodie,Sasaki, N. André,Boullier, Agnès,Sonnet, Pascal
, p. 702 - 722 (2016/07/26)
An important part of pathogenesis of Alzheimer's disease (AD) is attributed to the contribution of AGE (Advanced Glycation Endproducts) and ALE (Advanced Lipid peroxidation Endproducts). In order to attenuate the progression of AD, we designed a new type of molecules that consist of two trapping parts for reactive carbonyl species (RCS) and reactive oxygen species (ROS), precursors of AGE and ALE, respectively. These molecules also chelate transition metals, the promoters of ROS formation. In this paper, synthesis of the new AGE/ALE inhibitors and evaluation of their physicochemical and biological properties (carbonyl trapping capacity, antioxidant activity, Cu2+-chelating capacity, cytotoxicity and protective effect against in?vitro MGO-induced apoptosis in the model AD cell-line PC12) are described. It is found that compounds 40b and 51e possess promising therapeutic potentials for treating AD.
Synthesis, physicochemical properties, and biological evaluation of N- substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: Orally active iron chelators with clinical potential
Dobbin,Hider,Hall,Taylor,Sarpong,Porter,Xiao,Van der Helm
, p. 2448 - 2458 (2007/10/02)
The synthesis of a range of novel bidentate ligands containing the chelating moiety 3-hydroxy-4(1H)-pyridinone is described. The pK(a) values of the ligands and the stability constants of their iron(III) complexes have been determined. The crystal structures of one of the ligands and one of the iron(III) complexes are presented. The distribution coefficients of the ligands are reported and are related to the ability of the ligands to remove iron from hepatocytes. The influence of 3-hydroxy-4(1H)-pyridinones on oxidative damage to cells is described. In contrast to the iron chelator in current therapeutic use, desferrioxamine-B, many of the bidentate ligands described in this study are orally active in iron-overloaded mice.
