Synthesis and Aldose Reductase Inhibitory Activity of 2-Substituted 6-Fluoro-2,3-dihydrospiro[4H-1-benzopyran-4,4'-imidazolidine]2', 5'-diones

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Optically active and racemic 2-substituted 6-fluoro-2,3-dihydrospiro[4H-1-benzopyran-4,4'-imidazolidine]-2', 5'-diones were synthesized stereoselectively from (+)-, (-)-, and (±)-6-fluoro-3,4-dihydro-4-oxo-2H-1-benzopyran-2-carboxylic acid [(+)-1,(-)-1,and (±)-1], respectively, for evaluation as new aldose reductase inhibitors. Among these compounds, the 2S, 4S compounds were found to be more potent inhibitors of aldose reductase in vitro and in vivo than the corresponding 2R, 4R enantiomers. The chloromethyl compound [(+)-5] showed highly potent activities in inhibiting cataract formation in the lenses and polyol accumulation in the sciatic nerve of rats.
公益社団法人日本薬学会の論文
1994-07-15