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• W2076160861 abstract "A novel and concise scheme has been developed successfully for the syntheses of N-substituted fagomine derivatives. The transformation of lactone (2) to 1,5-diol (3) was carried on with high yield (93–95%). The cyclization of 4 to 5 is a high stereoselective reaction (de value > 98%). It is disclosed that bulky substituent at N atom of the piperidine decreases the inhibition activity except those substituents having the ability of solvation or forming disulfide bond with M444 at the active site of α-glycosidase, which enhance the interaction with enzyme. Compounds with S-configuration at C-3 show greater activity than those with R-configuration. The structure–activity relationship study is also supported by molecular docking analysis." @default.
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• W2076160861 date "2014-04-01" @default.
• W2076160861 modified "2023-10-16" @default.
• W2076160861 title "A concise synthesis of N-substituted fagomine derivatives and the systematic exploration of their α-glycosidase inhibition" @default.
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• W2076160861 doi "https://doi.org/10.1016/j.ejmech.2014.03.004" @default.
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