ArticleMolecules (Basel, Switzerland)2015
Multigram synthesis and in vivo efficacy studies of a novel multitarget anti-Alzheimer's compound.
Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- 4,4'-methylenediphenol reduces Aβ-induced toxicity in aFrontiers in aging neuroscience · 2024Article
- Amyloid β and Alzheimer's Disease: Molecular Updates from Physiology to Pathology.International journal of molecular sciences · 2023Article
- A novel rhein-huprine hybrid ameliorates disease-modifying properties in preclinical mice model of Alzheimer's disease exacerbated with high fat diet.Cell & bioscience · 2023Article
- On the interaction of a donepezil-huprine hybrid with synthetic membrane models.Neural regeneration research · 2023Article
- The separation of several organophosphate pesticides on immobilized polysaccharide chiral stationary phases.Chirality · 2022Article
- Protective Role of a Donepezil-Huprine Hybrid against the β-Amyloid (1-42) Effect on Human Erythrocytes.International journal of molecular sciences · 2021Article
- Ingredients in Zijuan Pu'er Tea Extract Alleviate β-Amyloid Peptide Toxicity in aMolecules (Basel, Switzerland) · 2019Article
- Neuroprotective Effects of the Multitarget Agent AVCRI104P3 in Brain of Middle-Aged Mice.International journal of molecular sciences · 2018Article
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Authors and funding
17 authors.
Funding
Abstract
We describe the multigram synthesis and in vivo efficacy studies of a donepezil‒huprine hybrid that has been found to display a promising in vitro multitarget profile of interest for the treatment of Alzheimer's disease (AD). Its synthesis features as the key step a novel multigram preparative chromatographic resolution of intermediate racemic huprine Y by chiral HPLC. Administration of this compound to transgenic CL4176 and CL2006 Caenorhabditis elegans strains expressing human Aβ42, here used as simplified animal models of AD, led to a significant protection from the toxicity induced by Aβ42. However, this protective effect was not accompanied, in CL2006 worms, by a reduction of amyloid deposits. Oral administration for 3 months to transgenic APPSL mice, a well-established animal model of AD, improved short-term memory, but did not alter brain levels of Aβ peptides nor cortical and hippocampal amyloid plaque load. Despite the clear protective and cognitive effects of AVCRI104P4, the lack of Aβ lowering effect in vivo might be related to its lower in vitro potency toward Aβ aggregation and formation as compared with its higher anticholinesterase activities. Further lead optimization in this series should thus focus on improving the anti-amyloid/anticholinesterase activity ratio.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.