2019
DOI: 10.1016/j.neuropharm.2019.05.025
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New evidence for dual binding site inhibitors of acetylcholinesterase as improved drugs for treatment of Alzheimer's disease

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Cited by 76 publications
(53 citation statements)
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“…Positions with the best binding affinities (see Table S1 in Supplementary Materials are discussed below. The position of the nitrile 2b binding in the active site gorge of hAChE obtained by molecular docking is very close to that of its nitro group-containing analog 1b , as observed by X-ray crystallography [ 26 ]. The inhibitor molecule spans through the whole gorge and occupies both the PAS and active site ( Figure 2 A).…”
Section: Resultsmentioning
confidence: 58%
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“…Positions with the best binding affinities (see Table S1 in Supplementary Materials are discussed below. The position of the nitrile 2b binding in the active site gorge of hAChE obtained by molecular docking is very close to that of its nitro group-containing analog 1b , as observed by X-ray crystallography [ 26 ]. The inhibitor molecule spans through the whole gorge and occupies both the PAS and active site ( Figure 2 A).…”
Section: Resultsmentioning
confidence: 58%
“…Recently, we developed a new class of selective mammalian dual binding site AChE inhibitors with an acyclic and macrocyclic structure based on 1,3-bis[ω-(substituted benzylethylamino) alkyl]-6-methyluracils. In particular, novel 6-methyl uracil derivatives with ω-(substituted benzylethylamino) alkyl chains at the N atoms of the pyrimidine ring ( Figure 1 ) were reported as selective AChE inhibitors [ 25 , 26 ]. In these compounds, the substituted electron-withdrawing nitro-, trifluoro-, and fluoro-group benzylethylamino moieties were bridged to N atoms of the 6-methyluracil moiety via various polymethylene chains.…”
Section: Introductionmentioning
confidence: 99%
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“…In this regard, hybrid anti-cholinesterase molecules were created in the form of multi-target ligands against AD. In this respect, hybrids were obtained, such as tacrine hybrids, whose selectivity over cholinesterase inhibition is markedly superior to tacrine, agents whose molecules have also demonstrated the ability to cross the BBB [96,97]. The BBB acts as a dynamic interface between the CNS and peripheral tissues, this barrier becoming a therapeutic target for providing drugs needed for neuropsychiatric disorders such as Alzheimer's dementia.…”
Section: Synthetic Analoguesmentioning
confidence: 99%