pyrimidinones and zopolrestat

pyrimidinones has been researched along with zopolrestat* in 1 studies

Other Studies

1 other study(ies) available for pyrimidinones and zopolrestat

Article	Year
Highly selective aldose reductase inhibitors. 3. Structural diversity of 3-(arylmethyl)-2,4,5-trioxoimidazolidine-1-acetic acids. Journal of medicinal chemistry, 1997, Feb-28, Volume: 40, Issue:5 Accumulation of intracellular sorbitol, the reduced product of glucose, catalyzed by aldose reductase (AR) (EC 1.1.1.21), is thought to be the cause of the development of diabetic complications. Our attention is focused on finding compounds which inhibit AR without significantly inhibiting aldehyde reductase (ALR) (EC 1.1.1.2). The uracil or 2,4-dioxoimidazolidine skeleton having the benzothiazolyl or 4-chloro-3-nitrophenyl group as an aryl part indicated not only extremely high AR inhibitory activity but also AR selectivity. The ratio of IC50(ALR)/IC50(AR) of 3-[(5-chlorobenzothiazol-2-yl)methyl]-1,2,3,4-tetrahydro-2,4- dioxopyrimidine-1-acetic acid (47d) was more than 17 500. The uracil skeleton with the benzothiazolyl moiety seemed to be the best combination for selective AR inhibition. Topics: Acetates; Aldehyde Reductase; Animals; Benzothiazoles; Diabetes Complications; Enzyme Inhibitors; Humans; Imidazoles; Kidney; Lens, Crystalline; Magnetic Resonance Spectroscopy; Models, Molecular; Molecular Structure; Phthalazines; Pyrimidinones; Rats; Sorbitol; Structure-Activity Relationship; Thiazoles	1997

Article

Year

Highly selective aldose reductase inhibitors. 3. Structural diversity of 3-(arylmethyl)-2,4,5-trioxoimidazolidine-1-acetic acids.

Journal of medicinal chemistry, 1997, Feb-28, Volume: 40, Issue:5

Accumulation of intracellular sorbitol, the reduced product of glucose, catalyzed by aldose reductase (AR) (EC 1.1.1.21), is thought to be the cause of the development of diabetic complications. Our attention is focused on finding compounds which inhibit AR without significantly inhibiting aldehyde reductase (ALR) (EC 1.1.1.2). The uracil or 2,4-dioxoimidazolidine skeleton having the benzothiazolyl or 4-chloro-3-nitrophenyl group as an aryl part indicated not only extremely high AR inhibitory activity but also AR selectivity. The ratio of IC50(ALR)/IC50(AR) of 3-[(5-chlorobenzothiazol-2-yl)methyl]-1,2,3,4-tetrahydro-2,4- dioxopyrimidine-1-acetic acid (47d) was more than 17 500. The uracil skeleton with the benzothiazolyl moiety seemed to be the best combination for selective AR inhibition.

Topics: Acetates; Aldehyde Reductase; Animals; Benzothiazoles; Diabetes Complications; Enzyme Inhibitors; Humans; Imidazoles; Kidney; Lens, Crystalline; Magnetic Resonance Spectroscopy; Models, Molecular; Molecular Structure; Phthalazines; Pyrimidinones; Rats; Sorbitol; Structure-Activity Relationship; Thiazoles

1997