Sharma, Piyoosh published the artcileDesign and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer’s disease, Application In Synthesis of 86-51-1, the main research area is phenylmethylidene benzyl piperidinamine preparation docking acetylcholinesterase secretase inhibition SAR; dibenzylpiperidinamine preparation docking acetylcholinesterase secretase inhibition SAR; Acetylcholinesterase (AChE); Alzheimer’s disease; Aβ aggregation; Multitarget-directed ligands; Structure-based drug design; β-Secretase-1 (BACE-1).
A series of N-benzylpiperidine analogs I and II [R = H, 4-F, 2,3-(MeO)2, etc.] were designed and synthesized as multi-functional inhibitors of acetylcholinesterase (AChE) and β-secretase-1 (BACE-1) with moderate to excellent inhibitory activities. Among the tested inhibitors, I and II [R = 4-O2N, 4-F3C] presented the most significant and balanced inhibition against both the targets. Compounds I [R = 4-O2N, 4-F3C] exhibited high brain permeability in the PAMPA-BBB assay, significant displacement of propidium iodide from the peripheral anionic site (PAS) of AChE and were devoid of neurotoxicity towards SH-SY5Y neuroblastoma cell lines up to the maximum tested concentration of 80 μM. Meanwhile, both these compounds inhibited self- and AChE-induced Aβ aggregation in thioflavin T assay, which was also re-affirmed by morphol. characterization of Aβ aggregates using at. force microscopy (AFM). Moreover, I [R = 4-O2N, 4-F3C] ameliorated the scopolamine-induced cognitive impairment in elevated plus and Y-maze experiments Ex-vivo and biochem. anal. established the brain AChE inhibitory potential and antioxidant properties of these compounds Further, improvement in Aβ1-42-induced cognitive impairment was also observed by compound I [R = 4-F3C] in the Morris water maze experiment with significant oral absorption characteristics ascertained by the pharmacokinetic studies.
European Journal of Medicinal Chemistry published new progress about Acute toxicity. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application In Synthesis of 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem