2019
DOI: 10.1002/slct.201803222
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Novel Coumarin‐Quinoline Hybrids: Design of Multitarget Compounds for Alzheimer's Disease

Abstract: Alzheimer's disease (AD) is the most prevalent neurodegenerative disease, presenting the most devastating consequences on human health and life quality. Coumarin‐quinoline hybrids were synthesized following a very efficient and versatile strategy. Small structural variations contributed to dual acetyl/butyrylcholinesterases (AChE/BuChE) activity or selectivity towards one of these enzymes. In addition, some of the studied compounds are interesting iron chelators, presenting a tendency to be neuroprotective. Mo… Show more

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Cited by 27 publications
(20 citation statements)
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“…These compounds showed high selectivity against acetylcholinesterase (AChE), and were also excellent iron chelating agents, with the most active compound against AChE exhibiting an IC50 of 159 µM. Remarkably, docking analysis (on the basis of the binding energy calculation), predicted the activity of these compounds, showing that the most active molecule of this new series had the best energy score [19]. Other compounds like dyhidropyrano[c]chromene derivatives have been used as cognitive enhancers in the treatment of different NDD [38].…”
Section: A Safer Approach To Ndd Drug Discovery: Green Chemistry Techmentioning
confidence: 98%
See 1 more Smart Citation
“…These compounds showed high selectivity against acetylcholinesterase (AChE), and were also excellent iron chelating agents, with the most active compound against AChE exhibiting an IC50 of 159 µM. Remarkably, docking analysis (on the basis of the binding energy calculation), predicted the activity of these compounds, showing that the most active molecule of this new series had the best energy score [19]. Other compounds like dyhidropyrano[c]chromene derivatives have been used as cognitive enhancers in the treatment of different NDD [38].…”
Section: A Safer Approach To Ndd Drug Discovery: Green Chemistry Techmentioning
confidence: 98%
“…In this review, we highlight the importance of using both, experimental and theoretical approaches such as green chemistry and molecular modeling, aimed to the rational drug design targeting NDD. Our multidisciplinary research team is working in different institutions and countries, tackling the lack of active and effective compounds against NDD, by synthesizing active molecules such as tetrahydroquinolines [17], diN-substituted glycyl-phenylalanine derivatives [18], coumarin-quinoline hybrids [19], aryl-1, 2, 3-triazolyl benzylpiperidines [20], indolylpiperidines [21], and glycogen synthase kinase-3 (GSK3) and tau-aggregation inhibitors [22], among others. These novel active molecules have been obtained by using a combination of green chemistry protocols, predictive chemoinformatics tools, and molecular modeling approaches.…”
Section: Introductionmentioning
confidence: 99%
“…In this field, recent studies designed and synthesized dihydropyrimidine and quinazoline bicycle as selective inhibitors against AChE enzyme . Likewise, quinolinyl chalcones derivatives exhibited selective inhibition for BChE enzyme displayed significant inhibition for AChE, Similarly, cumarine‐quinolines compounds showed ACHE selective inhibition . The change of functional groups in basic structure demonstrated variance in inhibition potential against BChE and AChE …”
Section: Introductionmentioning
confidence: 96%
“…[18][19][20] Moreover, hybrid molecules bearing the coumarin scaffold have been already reported by the group. [21,22] Therefore, the development of coumarin-rasagiline hybrids, and the methodology and results described in this manuscript, may contribute to a global effort to find efficient molecules as future perspectives for the treatment of Parkinson's disease (Figure 1).…”
Section: Introductionmentioning
confidence: 99%