Chiral Resolution of (1, 2-benzothiazin-4-yl)Acetic Acid Enantiomers as Aldose Reductase Inhibitors

摘要

Two novel (1, 2-benzothiazin-4-yl)acetic acid enantiomers were prepared by chiral resolution, and their enantiomeric purity was tested by chiral HPLC. The biological evaluation of the racemate and the single enantiomers showed that the isomer (R)-(-)-4 was the most active with an IC_(50) value of 0.120μM, which was 35 times more active than the other isomer (S)-(+)-4, indicating an important effect of C4 position on both the activity and selectivity.