A series of hydroxy- and hydroxy-methoxychalcones was synthesized and the inhibitory activity and selectivity of the compounds towards bovine lens aldose reductase (AR) were tested. All the compounds display affinity for AR The most active proved to be 1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)propen-1-one (isoliquiritigenin, IC50 = 7.60 mu M). The selectivity of this compound was also tested, its inhibitory activity being assayed against glutathione reductase and sorbitol dehydrogenase
Synthesis and description of chalcone-like compounds, inhibitors of aldose reductase / Severi, F; Costantino, Luca; Benvenuti, Stefania; Vampa, Gabriella; Mucci, Adele. - In: MEDICINAL CHEMISTRY RESEARCH. - ISSN 1054-2523. - STAMPA. - 6:(1996), pp. 128-136.
Synthesis and description of chalcone-like compounds, inhibitors of aldose reductase
COSTANTINO, Luca;BENVENUTI, Stefania;VAMPA, Gabriella;MUCCI, Adele
1996
Abstract
A series of hydroxy- and hydroxy-methoxychalcones was synthesized and the inhibitory activity and selectivity of the compounds towards bovine lens aldose reductase (AR) were tested. All the compounds display affinity for AR The most active proved to be 1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)propen-1-one (isoliquiritigenin, IC50 = 7.60 mu M). The selectivity of this compound was also tested, its inhibitory activity being assayed against glutathione reductase and sorbitol dehydrogenase
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