Chalcones as Potential Inhibitors of Aldose Reductase

Page: 320

M. Chlupacovaa and V. Opletalovab

aDepartment of Pharmaceutical Chemistry and Drug Control, bResearch Centre LN00B125, Faculty of Pharmacy, Charles University, Hradec Kralove


Chalcone (1,3-diphenylprop-2-en-1-one) and its derivatives show numerous biological activities. In this review, their effects on aldose reductase, the enzyme that plays an important role in pathogenesis of secondary diabetic complications, are described. The highest potency was observed for derivatives with hydroxy derivatives in positions 2 and 4 of ring A, whilst the substitution pattern in the other ring seems to be less important. Structure - activitity studies have also revealed that the presence of the enone grouping is not necessary for the inhibition of aldose reductase. Hence, corresponding dihydrochalcones could be used to prevent possible side effects resulting from the high reactivity of the enone grouping.


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