Synthesis and aldose reductase inhibitory activity of<i>N</i>-1,<i>N</i>-4-disubstituted 3,4-dihydro-2(1<i>H</i>)-quinoxalinone derivatives
作者:Reinhard Sarges、John W. Lyga
DOI:10.1002/jhet.5570250543
日期:1988.9
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
已经开发出用于制备4-酰化的,4-苯磺酰化的和4-甲基化的3,4-二氢-2(1H)-喹喔啉酮-1-乙酸的合成路线。还制备了相应的丙酸的一个实例。已经评估了这些化合物在体外抑制牛晶状体醛糖还原酶的能力。该系列的某些成员在体内也显示弱活性,抑制链脲佐菌素-糖尿病大鼠坐骨神经中的山梨醇形成。