Chiral resolution, determination of absolute configuration, and biological evaluation of (1,2-benzothiazin-4-yl)acetic acid enantiomers as aldose reductase inhibitors

β-Aldehyde ketones as dual inhibitors of aldose reductase and α-glucosidase with antioxidant properties

“…2 Although the pathogenesis of diabetic complications is generally complex and substantial, previous experimental and clinical measurements have demonstrated that the activation of the polyol pathway and the resulting oxidative stress are the main causes of diabetic complications. [3][4][5] Therefore, the goal in the treatment of DM is a reduction in blood glucose levels and control of any subsequent complications.…”

Novel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity

“…Based on our previous work of structurally different ARIs 19–22 , we have engaged in preparing a novel series of 2-phenoxypyrido[3,2- b ]pyrazin-3(4 H )-one derivatives as the new multifunctional ARIs with combined AKR1B1 inhibition and antioxidant activity. This study will focus on the further optimisation of the C2 side chain and the introduction of halogen substituent to the C7 position of the core structure.…”

Aromatic Heterobicyclics-Based Design of Aldose Reductase Inhibitors as Drug Candidates for the Treatment of Diabetic Complications

“…In the benzothiazine series including compounds 3-4, the orientation of the carboxylic acid head is likely to have a strong influence on the interaction between the ALR2 and inhibitors. Z-isomers of 3 is more active than E-isomers, [11] while R-(−)-enantiomers of 4 (IC 50 =500 M) than S-(+)-enantiomers (IC 50 =4150 nM) [10,19] (Table 2).…”