《Synthesis and in vitro evaluation of vanillin derivatives as multi-target therapeutics for the treatment of Alzheimer’s disease》 was written by Blaikie, Laura; Kay, Graeme; Kong Thoo Lin, Paul. Product Details of 51857-17-1This research focused onvanillin naphthalimido phthalimido preparation Alzheimer agent mol modeling; cholinesterase inhibitor naphthalimido phthalimido vanillin; Alzheimer’s disease; Antioxidant; Binding conformation; Cholinesterase inhibitor; Multi-target strategy; Vanillin derivatives. The article conveys some information:
A number of novel naphthalimido and phthalimido vanillin derivatives were synthesized, and evaluated as antioxidants and cholinesterase inhibitors in vitro. Antioxidant activity was assessed using DPPH, FRAP, and ORAC assays. All compounds demonstrated enhanced activity compared to the parent compound, vanillin. They also exhibited BuChE selectivity in Ellman’s assay. A lead compound, naphthalimido derivative I, was identified and displayed strong antioxidant activity (IC50 of 16.67μM in the DPPH assay, a 25-fold increase in activity compared to vanillin in the FRAP assay, and 9.43 TE in the ORAC assay). Furthermore, I exhibited potent BuChE selectivity, with an IC50 of 0.27μM which was around 53-fold greater than the corresponding AChE inhibitory activity. Mol. modeling studies showed that mols. with bulkier groups, as in I, exhibited better BuChE selectivity. This work provides a promising basis for the development of multi-target hybrid compounds based on vanillin as potential AD therapeutics. After reading the article, we found that the author used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Product Details of 51857-17-1
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