Aldose reductase inhibition by 2,4-oxo and thioxo derivatives of 1,2,3,4-tetrahydroquinazoline

Article abstract of DOI:10.1016/0223-5234(90)90019-Y

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 andto prevent cataract formation.