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- W173889209 abstract "Inhibitors of aldose reductase are believed to be useful for the treatment of diabetic complications. Original [(2,4-dioxo-1,2,3,4-tetrahydro)quinazolin-1-yl] acetic acids and their thioxo derivatives have been synthesized and examined for their ability to inhibit aldose reductase in vitro and in vivo. Most were active in vitro on rat lens aldose reductase in the 10−7 molar range. Compound V16, which has a (2′-fluoro-4′-bromo)benzyl substituent on nitrogen N-3 was found in hypergalactosemic rats to be a good inhibitor of galactitol accumulation in sciatic nerves and to prevent cataract formation. Les inhibiteurs de l'aldose réductase sont des candidats potentiels pour le traitement des complications diabétiques. Des dérivés originaux de l'acide [(2,4-dioxo ou thioxo 1,2,3,4-tétrahydro)quinazolin-1-yl] acétique ont été préparés et leur activité inhibitrice de l'aldose réductase a été étudiée in vitro et in vivo. La plupart de ces composés sont actifs in vitro à 10−7 mol sur l'aldose réductase du cristallin de rat. Le composé V16, qui possède un substituant (2′-fluoro-4′-bromo)benzyle sur l'azote en 3 de la quinazoline inhibe l'accumulation du galactitol dans le nerf sciatique et prévient la formation de cataracte chez le rat soumis à un régime enrichi en galactose." @default.
- W173889209 created "2016-06-24" @default.
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- W173889209 date "1990-03-01" @default.
- W173889209 modified "2023-09-27" @default.
- W173889209 title "L'inhibition de l'aldose réductase par des dérivés 2,4-oxo et thioxo de la 1,2,3,4-tétrahydro quinazoline" @default.
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- W173889209 doi "https://doi.org/10.1016/0223-5234(90)90019-y" @default.
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