Inhibition of amyloid-β aggregation by coumarin analogs can be manipulated by functionalization of the aromatic center

Soto-Ortega, Deborah D.; Murphy, Brandon P.; Gonzalez-Velasquez, Francisco J.; Wilson, Kelly A.; Xie, Fang; Wang, Qin; Moss, Melissa A.

doi:10.1016/j.bmc.2011.03.010

Cited by 90 publications

(49 citation statements)

References 48 publications

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“…46 Importantly, these derivatives have been frequently reported to be inhibitors of Aβ aggregation, and might therefore provide advantageous anti-aggregatory activity. 47,48 …”

Section: Designmentioning

confidence: 98%

“…Several small molecules that contain different aromatic centers, namely coumarine, benzoxazole, and benzothiazole (and some others), can prevent this self-induced aggregation of Aβ peptides by disrupting the π stacking of the aromatic residues in the process of Aβ aggregate formation. Molecular entities with such aromatic centers might present a promising approach for the development of novel neuroprotective agents, particularly when combined with additional anti-AD activities 47,48,56. Aβ 1-42 was used as a model peptide, as it is…”

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confidence: 99%

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Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

Knez

Brus

Coquelle

et al. 2015

Bioorganic & Medicinal Chemistry

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“…46 Importantly, these derivatives have been frequently reported to be inhibitors of Aβ aggregation, and might therefore provide advantageous anti-aggregatory activity. 47,48 …”

Section: Designmentioning

confidence: 98%

mentioning

confidence: 99%

Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

Knez

Brus

Coquelle

et al. 2015

Bioorganic & Medicinal Chemistry

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“…23 Thus, some BTA derivatives have been used as Alzheimer's brain imaging agents 24 , while others have evidenced capacity for the peptide aggregation and neuro-protective roles. 25,26 More recently quite a number of studies have been focused on the development of therapeutic strategies multitarget drugs to fight multifactorial neurodegenerative disorders, such as AD. Thus, one of the most explored design strategies has been focused on the development of hybrids that combine the ChEs inhibition role, for the enhancement of the cholinergic neurotransmission, with other relevant roles (eg reduction the Aβ fibril self-aggregation, antioxidant and metal depletion).…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis and neuroprotective evaluation of novel tacrine–benzothiazole hybrids as multi-targeted compounds against Alzheimer’s disease

Keri¹,

Quintanova²,

Marques³

et al. 2013

Bioorganic & Medicinal Chemistry

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“…The main phenolic component of olive oil, oleuropein, has been shown to possess antioxidant [262] , anti-inflammatory [263] and hypolipidemic activities [264] . Small molecules (NQTrp, ClNQTrp, coumarin, furosemide, D737) that inhibit Aβ aggregation [265,266] or remodel toxic soluble oligomers of Aβ [267] inhibit oligomer formation [268][269][270][271][272][273][274] (Table 3).…”

Section: Small Molecule Inhibitorsmentioning

confidence: 99%

Amyloid beta: structure, biology and structure-based therapeutic development

et al. 2017

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Amyloid beta peptide (Aβ) is produced through the proteolytic processing of a transmembrane protein, amyloid precursor protein (APP), by β-and γ-secretases. Aβ accumulation in the brain is proposed to be an early toxic event in the pathogenesis of Alzheimer's disease, which is the most common form of dementia associated with plaques and tangles in the brain. Currently, it is unclear what the physiological and pathological forms of Aβ are and by what mechanism Aβ causes dementia. Moreover, there are no efficient drugs to stop or reverse the progression of Alzheimer's disease. In this paper, we review the structures, biological functions, and neurotoxicity role of Aβ. We also discuss the potential receptors that interact with Aβ and mediate Aβ intake, clearance, and metabolism. Additionally, we summarize the therapeutic developments and recent advances of different strategies for treating Alzheimer's disease. Finally, we will report on the progress in searching for novel, potentially effective agents as well as selected promising strategies for the treatment of Alzheimer's disease. These prospects include agents acting on Aβ, its receptors and tau protein, such as small molecules, vaccines and antibodies against Aβ; inhibitors or modulators of β-and γ-secretase; Aβ-degrading proteases; tau protein inhibitors and vaccines; amyloid dyes and microRNAs.

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Inhibition of amyloid-β aggregation by coumarin analogs can be manipulated by functionalization of the aromatic center

Cited by 90 publications

References 48 publications

Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

Design, synthesis and neuroprotective evaluation of novel tacrine–benzothiazole hybrids as multi-targeted compounds against Alzheimer’s disease

Amyloid beta: structure, biology and structure-based therapeutic development

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