Evaluation of the Hepatoprotective Effect of L-Ascorbate 1-(2-Hydroxyethyl)-4,6-Dimethyl-1,2-Dihydropyrimidine-2-One Upon Exposure to Carbon Tetrachloride

© 2017, Springer Science+Business Media New York.Hepatoprotective properties of a new pyrimidine derivative — L-ascorbate 1-(2-hydroxyethyl)-4,6-dimethyl-1,2-dihydropyrimidine-2-one, synthesized on the basis Xymedon, were assessed in white rats exposed to CCl4. The compound under study administered prior to exposure to CCl4 reduced the deviation of biochemical parameters from reference values and severity of structural and morphological changes in liver, when compared to the control. Hepatoprotective properties of the studied compound were more pronounced than those of Xymedon

Study of hepatoprotective effects of xymedon

Xymedon (1-(β-oxyethyl)-4,6-dimethyl-1,2-dihydro-2-oxopyrimidine), a regeneratory and wound-healing drug, exhibited hepatoprotective activity in laboratory animals with experimental toxic hepatitis. Oral drug reduced the severity of toxic involvement of the liver induced by CCl4 and reduced animal mortality. Xymedon promoted recovery of the blood biochemical parameters characterizing the liver status. © 2013 Springer Science+Business Media New York

Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase

© the Partner Organisations 2014. Novel pyrimidinophanes possessing two o-nitrobenzylethyldialkylammonium heads bridging with different spacers were prepared. Pyrimidinophanes 2a, 2b and 3 are reversible inhibitors of cholinesterases. They show a very good selectivity for human acetylcholinesterase (AChE), with an inhibitory power 100-200 times higher than for human butyrylcholinesterase (BChE). Docking simulations indicate specific binding of pyrimidinophanes 2a and 4 onto the peripheral anionic site of AChE. Other compounds bind to the active center of AChE as well as to the peripheral anionic site. These compounds are dual binding site inhibitors. Pyrimidinophane 2b and its acyclic counterpart 1 were tested in the animal model of myasthenia gravis and may be considered as valuable candidates for the treatment of pathological muscle weakness syndromes. This journal i

6-methyluracil derivatives as bifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease

© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Novel 6-methyluracil derivatives with ω-(substituted benzylethylamino)alkyl chains at the nitrogen atoms of the pyrimidine ring were designed and synthesized. The numbers of methylene groups in the alkyl chains were varied along with the electron-withdrawing substituents on the benzyl rings. The compounds are mixed-type reversible inhibitors of cholinesterases, and some of them show remarkable selectivity for human acetylcholinesterase (hAChE), with inhibitory potency in the nanomolar range, more than 10 000-fold higher than that for human butyrylcholinesterase (hBuChE). Molecular modeling studies indicate that these compounds are bifunctional AChE inhibitors, spanning the enzyme active site gorge and binding to its peripheral anionic site (PAS). In vivo experiments show that the 6-methyluracil derivatives are able to penetrate the blood-brain barrier (BBB), inhibiting brain-tissue AChE. The most potent AChE inhibitor, 3 d (1,3-bis[5-(o-nitrobenzylethylamino)pentyl]-6-methyluracil), was found to improve working memory in scopolamine and transgenic APP/PS1 murine models of Alzheimer's disease, and to significantly decrease the number and area of β-amyloid peptide plaques in the brain. Head-AChE relief! In our efforts to identify compounds to treat Alzheimer′s disease, we found that 1,3-bis[ω-(substituted benzylethylamino)alkyl]-6-methyluracils bind to the active site gorge and peripheral anionic site of acetylcholinesterase (AChE). These compounds can cross the blood-brain barrier, and decrease the number and area of β-amyloid plaques in the brain

Evaluation of the Hepatoprotective Effect of L-Ascorbate 1-(2-Hydroxyethyl)-4,6-Dimethyl-1,2-Dihydropyrimidine-2-One Upon Exposure to Carbon Tetrachloride

© 2017, Springer Science+Business Media New York.Hepatoprotective properties of a new pyrimidine derivative — L-ascorbate 1-(2-hydroxyethyl)-4,6-dimethyl-1,2-dihydropyrimidine-2-one, synthesized on the basis Xymedon, were assessed in white rats exposed to CCl4. The compound under study administered prior to exposure to CCl4 reduced the deviation of biochemical parameters from reference values and severity of structural and morphological changes in liver, when compared to the control. Hepatoprotective properties of the studied compound were more pronounced than those of Xymedon

Evaluation of the Hepatoprotective Effect of L-Ascorbate 1-(2-Hydroxyethyl)-4,6-Dimethyl-1,2-Dihydropyrimidine-2-One Upon Exposure to Carbon Tetrachloride

© 2017, Springer Science+Business Media New York.Hepatoprotective properties of a new pyrimidine derivative — L-ascorbate 1-(2-hydroxyethyl)-4,6-dimethyl-1,2-dihydropyrimidine-2-one, synthesized on the basis Xymedon, were assessed in white rats exposed to CCl4. The compound under study administered prior to exposure to CCl4 reduced the deviation of biochemical parameters from reference values and severity of structural and morphological changes in liver, when compared to the control. Hepatoprotective properties of the studied compound were more pronounced than those of Xymedon

Evaluation of the Hepatoprotective Effect of L-Ascorbate 1-(2-Hydroxyethyl)-4,6-Dimethyl-1,2-Dihydropyrimidine-2-One Upon Exposure to Carbon Tetrachloride

© 2017, Springer Science+Business Media New York.Hepatoprotective properties of a new pyrimidine derivative — L-ascorbate 1-(2-hydroxyethyl)-4,6-dimethyl-1,2-dihydropyrimidine-2-one, synthesized on the basis Xymedon, were assessed in white rats exposed to CCl4. The compound under study administered prior to exposure to CCl4 reduced the deviation of biochemical parameters from reference values and severity of structural and morphological changes in liver, when compared to the control. Hepatoprotective properties of the studied compound were more pronounced than those of Xymedon

Study of hepatoprotective effects of xymedon

Xymedon (1-(β-oxyethyl)-4,6-dimethyl-1,2-dihydro-2-oxopyrimidine), a regeneratory and wound-healing drug, exhibited hepatoprotective activity in laboratory animals with experimental toxic hepatitis. Oral drug reduced the severity of toxic involvement of the liver induced by CCl4 and reduced animal mortality. Xymedon promoted recovery of the blood biochemical parameters characterizing the liver status. © 2013 Springer Science+Business Media New York

Study of hepatoprotective effects of xymedon

Xymedon (1-(β-oxyethyl)-4,6-dimethyl-1,2-dihydro-2-oxopyrimidine), a regeneratory and wound-healing drug, exhibited hepatoprotective activity in laboratory animals with experimental toxic hepatitis. Oral drug reduced the severity of toxic involvement of the liver induced by CCl4 and reduced animal mortality. Xymedon promoted recovery of the blood biochemical parameters characterizing the liver status. © 2013 Springer Science+Business Media New York

Study of hepatoprotective effects of xymedon

Xymedon (1-(β-oxyethyl)-4,6-dimethyl-1,2-dihydro-2-oxopyrimidine), a regeneratory and wound-healing drug, exhibited hepatoprotective activity in laboratory animals with experimental toxic hepatitis. Oral drug reduced the severity of toxic involvement of the liver induced by CCl4 and reduced animal mortality. Xymedon promoted recovery of the blood biochemical parameters characterizing the liver status. © 2013 Springer Science+Business Media New York