2017
DOI: 10.1016/j.bmcl.2016.11.065
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Design and synthesis of new piperidone grafted acetylcholinesterase inhibitors

Abstract: Alzheimer’s disease (AD) is a neurodegenerative disorder affecting 35 million people worldwide. A common strategy to improve the well-being of AD patients consists on the inhibition of acetylcholinesterase with the concomitant increase of the neurotransmitter acetylcholine at cholinergic synapses. Two series of unreported N-benzylpiperidines 5(a–h) and thiazolopyrimidines 9(a–q) molecules were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) inhibitory activities. Among the newly synthe… Show more

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Cited by 27 publications
(16 citation statements)
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“…Currently, non-viral vectors have been widely used for gene therapy, but carrier toxicity is an important problem in the clinical application of non-viral vectors, usually due to their positively charged surface [32,33]. In our study, Tf-PL/AChE has a particle size of 113.0 ± 5.2 nm, a PDI of 0.113, and a potential of 28.5 mV, and these features confer its use for intravenous administration.…”
Section: Discussionmentioning
confidence: 71%
See 1 more Smart Citation
“…Currently, non-viral vectors have been widely used for gene therapy, but carrier toxicity is an important problem in the clinical application of non-viral vectors, usually due to their positively charged surface [32,33]. In our study, Tf-PL/AChE has a particle size of 113.0 ± 5.2 nm, a PDI of 0.113, and a potential of 28.5 mV, and these features confer its use for intravenous administration.…”
Section: Discussionmentioning
confidence: 71%
“…Therefore, transferrin receptors can be a drug delivery target for liver cancer treatment. Acetyl cholinesterase (AChE) has many non-choline functions in addition to the classic function of neurotransmitter by breaking down the neurotransmitter Acetylcholine (ACh) [32,33]. Oncomine data showed extremely high expression of ACh in various tumor tissues including liver cancer, p = 0.002, ( Figure S2A, Supporting Information), while AChE showed signi cant low expression (p = 0.012, Figure S2B, Supporting Information).…”
Section: Introductionmentioning
confidence: 99%
“…Currently, non-viral vectors have been widely used for gene therapy [43,44]. In order to achieve targeted delivery of therapeutic drugs to tumor cells, receptor-mediated active targeting has been generally adopted in recent years, such as the presence of asialoglycoprotein receptors on liver parenchymal cell membranes; mannose receptors are distributed on non-parenchymal cell membranes.…”
Section: Cell Cycle and Apoptosis Studymentioning
confidence: 99%
“…Acetylcholinesterase (AChE) plays key role in the cholinergic system, and its dysregulation is involved in a variety of human diseases [42]. AChE can degrade the ACh and reduce the malignant development risk of liver cancer, thus AChE has been identi ed as a prognostic marker in liver cancer [41,43,44]. Oncomine database shows extremely high expression of ACh in various tumor tissues including liver cancer, p=0.002 ( Figure S3), while AChE shows signi cant low expression in liver cancer p=0.012 ( Figure S4).…”
mentioning
confidence: 99%
“…We can expect that the number of patients will increase in the future in line with increasing population longevity . In view of the failures of therapeutics in different stages of clinical trials, the commonly known prevalence data call for elucidation of the pathological mechanism .…”
mentioning
confidence: 99%