71267-12-4Relevant academic research and scientific papers
An expeditious access to 5-pyrimidinol derivatives from cyclic methylglyoxal diadducts, formation of argpyrimidines under physiological conditions and discovery of new CFTR inhibitors
Renard, Brice-Lo?c,Boucherle, Benjamin,Maurin, Bruno,Molina, Marie-Carmen,Norez, Caroline,Becq, Frédéric,Décout, Jean-Luc
experimental part, p. 1935 - 1941 (2011/05/02)
In the study of previously reported modulators of CFTR chloride channels that are cyclic methylglyoxal (MG) diadducts (CMGD) to aromatic α-aminoazaheterocycles, we optimized a new expeditious one pot route for preparing in water novel aromatic polycyclic azaheterocycles and described 5-pyrimidinols antioxidants through the formation of 2-oxoaldehyde diadducts to aromatic α-aminoazaheterocycles, amidines, guanidines and thiourea. In regard to the importance as biomarkers of diabetic complications of the 5-pyrimidinols "argpyrimidines" formed in proteins from MG and arginine residues, we demonstrated that argpyrimidines are slowly formed under physiological conditions from CMGD to arginine derivatives according to the synthesis route described. Among the 5-pyrimidinol derivatives prepared, two polycyclic derivatives appeared to inhibit strongly the activity of CFTR channels in wt-CHO cells.
The Effect of Ring Nitrogen Atoms on the Homolytic Reactivity of Phenolic Compounds: Understanding the Radical-Scavenging Ability of 5-Pyrimidinols
Valgimigli, Luca,Brigati, Giovanni,Pedulli, Gian Franco,DiLabio, Gino A.,Mastragostino, Marina,Arbizzani, Catia,Pratt, Derek A.
, p. 4997 - 5010 (2007/10/03)
Six substituted 5-pyrimidinols were synthesized, and the thermochemistry and kinetics of their reactions with free radicals were studied and compared to those of equivalently substituted phenols. To assess their potential as hydrogen-atom donors to free r
Novel chain-breaking antioxidants
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, (2008/06/13)
Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.
