1450832-95-7

Upstream product

• 69567-11-9 2,3,4,6-tetra-O-benzyl-1,5-dideoxy-1,5-imino-D-glucitol 
• 1450832-94-6 2-(4-((2R,3R,4R,5S)-3,4,5-tris(benzyloxy)-2-((benzyloxy)methyl)piperidin-1-yl)butyl)isoindoline-1,3-dione 

Downstream Products

• 1450833-19-8 C₁₉H₃₀N₂O₅S 
• 1450833-22-3 C₁₉H₂₇F₃N₂O₅ 
• 1450833-24-5 C₁₉H₃₀N₂O₆ 
• 1450833-26-7 C₁₉H₂₇F₃N₂O₅ 
• 1450833-28-9 C₁₈H₂₈N₂O₆ 
• 1450833-30-3 C₁₉H₃₀N₂O₆ 
• 1450833-32-5 C₁₈H₂₉N₃O₅ 
• 1450833-34-7 C₁₈H₂₇FN₂O₅ 
• 1450833-36-9 C₁₉H₂₇F₃N₂O₅ 
• 1450833-38-1 C₂₀H₂₉ClN₂O₆ 
• 1450833-40-5 C₁₉H₃₀N₂O₆ 
• 1450833-42-7 C₁₈H₂₈N₂O₆ 
• 1450833-44-9 C₁₈H₂₉N₃O₅ 
• 1450833-46-1 C₁₈H₂₆F₂N₂O₅ 

Relevant academic research and scientific papers

Study on the synthesis and biological activities of N-alkylated deoxynojirimycin derivatives with a terminal tertiary amine

A series of N-alkylated deoxynojirimycin (DNJ) derivatives connected to a terminal tertiary amine at the alkyl chains of various lengths were prepared. These novel synthetic compounds were assessed for preliminary glucosidase inhibition and anticancer activities in vitro. Potent and selective inhibition was observed among them. Compound 7d (IC50 = 0.052 mM) showed improved and selective inhibitory activity against β-glucosidase compared to DNJ (IC50 = 0.65 mM). In addition, analysis of the kinetics of enzyme inhibition by using Lineweaver-Burk plots indicated that 7d inhibited β-glucosidase in a competitive manner, suggesting that 7d was expected to bind to the active site of β-glucosidase. Compounds 8b and 8c were found to be moderate and selective inhibitors of α-glucosidase. Nevertheless, none of compounds inhibited the growth of B16F10 melanoma cells.

Rapid modifications of N-substitution in iminosugars: Development of new β-glucocerebrosidase inhibitors and pharmacological chaperones for Gaucher disease

The rapid discovery of β-glucocerebrosidase (GCase) inhibitors and pharmacological chaperones for Gaucher disease is described. The N-aminobutyl DNJ-based iminosugar was synthesized and conjugating with a variety of carboxylic acids to generate a N-diversely substituted iminosugar-based library. Several members of this library were found to be nanomolar-range inhibitors of GCase; the inhibition constant Ki of the most potent was found to be 71 nM. Although these new molecules showed reasonable chaperoning activity (1.5- to 1.9-fold) in the N370S fibroblast of Gaucher patient-derived cell line, this was accompanies by a concomitant decrease in the cellular α-glucosidase activity, which might limit their further therapeutic potential. Next, newly developed N-substituents were assembled with pyrrolidine-based scaffolds to generate new molecules for further evaluation. The new 2,5-dideoxy-2,5-imino-d- mannitol (DMDP)-based iminosugar 22 was found to exhibit a satisfactory chaperoning activity to enhance GCase activity by 2.2-fold in Gaucher N370S cell line, without impairment of cellular α-glucosidase activity.