Synthesis and aldose reductase inhibitory activity of N-1,N-4-disubstituted 3,4-dihydro-2(1H)-quinoxalinone derivatives

Article abstract of DOI:10.1002/jhet.5570250543

Synthetic routes have been developed for the preparation of 4-acylated, 4-benzenesulfonylated, and 4-methylated 3,4-dihydro-2(1H)-quinoxalinone-1-acetic acids. One example of the corresponding propionic acid has also been made. These compounds have been evaluated for their ability to inhibit bovine lens aldose reductase in vitro. Some members from this series also show weak activity in vivo, inhibiting sorbitol formation in sciatic nerves of streptozotocin-diabetic rats.