Protein kinase C (PKC) and aldose reductase (AR) enzyme activities are increased in diabetes and complications are include retinopathy, nephropathy, and neuropathy. However, the relationship between PKC and AR and the underlying molecular mechanisms is still unclear. We aimed to evaluate the relationship between these two enzymes and clarify the underlying molecular mechanisms by the related signaling molecules.
View Article and Find Full Text PDFObjectives: To synthesize and characterize 2-[[6-(4-bromophenyl)imidazo[2,1-]thiazol-3-yl]acetyl]--alkyl/arylhydrazinecarbothioamide and 3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinone derivatives and evaluate them for their aldose reductase (AR) inhibitory effect.
Materials And Methods: 2-[[6-(4-bromophenyl)imidazo[2,1-]thiazol-3-yl]acetyl]--alkyl/arylhydrazinecarbothioamides () and 3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinones () were synthesized from 2-[6-(4-bromophenyl)imidazo[2,1-]thiazole-3-yl]acetohydrazide (). Their structures were elucidated by elemental analyses and spectroscopic data.
J Enzyme Inhib Med Chem
June 2008
Aldose reductase (AR) is implicated to play a critical role in diabetes and cardiovascular complications because of the reaction it catalyzes. AR enzyme appears to be the key factor in the reduction of glucose to sorbitol. Synthesis and accumulation of sorbitol in cells due to AR activity is the main cause of diabetic complications, such as diabetic cataract, retinopathy, neuropathy and nephropathy.
View Article and Find Full Text PDFA new series of flavonyl-2,4-thiazolidinediones (Va-c, VIa-c) was prepared by Knoevenagel reaction. The synthesized compounds were tested for their ability to inhibit rat kidney aldose reductase (AR) and for their insulinotropic activities in INS-1 cells. Compound Vb was able to increase insulin release in the presence of 5.
View Article and Find Full Text PDFAs it is known that still, there were no any confident ARIs on the market and they have several side effects, we need to approve new ARIs to reduce diabetic complications especially which have effect on the cataract formation. In this study, a new series of chromonyl-2,4-thiazolidinediones (Ia-e, IIa-e, IIIa-e) were prepared by Knoevenagel reaction with substituted 3-formylchromones (3a-e) and unsubstituted (1) or substituted 2,4-thiazolidinedione (2). The synthesized compounds were tested for their ability to inhibit rat kidney AR by an in vitro spectrophotometric assay.
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