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- W2391360240 abstract "Aim To synthesize methylquinolinoneacetic acids,and to assay their inhibitory activities against aldose reductase(AR).Methods The methylquinolinoneacetic acids were synthesized via addition,hydrolysis,cyclization,alkylation,condensation,and hydrolysis,a six-step procedure starting from methyl substituted aniline.Using epalrestat as a control,the aldose reductase inhibitory activities of the compounds obtained were evaluated on rat lens aldose reductase in vitro.Results Twenty-six compounds were obtained and all of them were not reported yet,and their structures were characterized by 1H-NMR and IR.Among the compounds tested,6-methylquinolinoneacetic acids show good activities,and compound Ⅵ6(IC50=0.088 μmol·L-1)exhibits the best activity,which is comparable with epalrestat;however,8-methylquinolinoneacetic acids are relatively weaker,only compounds Ⅵ15 and Ⅵ23 exert significant activities,the IC50 is 3.379 and 3.055 μmol·L-1 each.Conclusion The structure-activity relationships of methylquinolinoneacetic acids,as a novel type of aldose reductase inhibitor,should be investigated further." @default.
- W2391360240 created "2016-06-24" @default.
- W2391360240 creator A5086779479 @default.
- W2391360240 date "2009-01-01" @default.
- W2391360240 modified "2023-09-25" @default.
- W2391360240 title "Synthesis and aldose reductase inhibitory activities of methylquinolinoneacetic acids" @default.
- W2391360240 hasPublicationYear "2009" @default.
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