Synthesis and Aldose Reductase Inhibitory Activity of Triazine Derivatives Possessing Acetic Acid Group

概要

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N-Acetic acid derivatives of 6-aryl-pyrazolo-triazin-4-ones were synthesized for evaluation as new aldose reductase inhibitors. The intrinsic activity of each compound was assessed by measuring the inhibition of enzymatic activity in an isolated pig lens enzyme preparation. All the prepared compounds exhibited a significant in vitro aldose reductase inhibitory effect (10^<-6>M⩽IC_<50>⩽10^<-4>M). Furthermore, biological activity (log 1/IC_<50>) for most of the data sets could be correlated directly to electronic and steric parameters. Finally, spatial configuration of the most active derivative 6c (IC_<50>=2×10^<-6>M) was compared with that of tolrestat and with pharmacophor requirements of the aldose reductase inhibitor site using a molecular modeling system.
公益社団法人日本薬学会の論文
1992-06-25