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- W2373106987 abstract "Aim To discover new structure of β-secretase inhibitors.Methods Combining with Dock method and basing on the structural feature of active site of β-secretase binding to the typical inhibitors,isothiazolone substituted isophthalic acid derivatives were designed and synthesized.Time-resolved fluorescence(TRF) was used to evaluate the inhibitory activity of these compounds against β-secretase.Results Ten target compounds were synthesized and their structures were identified by MS and 1H-NMR.The purity of these compounds was determined by HPLC.Binding assay(TRF) showed that four of these ten compounds had obvious inhibitory activity against β-secretase.Especially,the IC50 value of compound 22a against β-secretase was 13.7 nmol·L-1.Conclusion New type β-secretase inhibitors were discovered.The preliminary structure-activity relationship concluding from this research will give a direction for the structural optimization of these β-secretase inhibitors." @default.
- W2373106987 created "2016-06-24" @default.
- W2373106987 creator A5053208897 @default.
- W2373106987 date "2010-01-01" @default.
- W2373106987 modified "2023-09-23" @default.
- W2373106987 title "Design,synthesis and inhibitory activity against β-secretase of isothiazolone substituted isophthalic acid derivatives" @default.
- W2373106987 hasPublicationYear "2010" @default.
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