100202-39-9Relevant articles and documents
Ferulic acid amide derivatives with varying inhibition of amyloid-β oligomerization and fibrillization
Kolaj, Igri,Wang, Yanfei,Ye, Kailin,Meek, Autumn,Liyanage, S. Imindu,Santos, Clarissa,Weaver, Donald F.
supporting information, (2021/07/07)
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized, in part, by the misfolding, oligomerization and fibrillization of amyloid-β (Aβ). Evidence suggests that the mechanisms underpinning Aβ oligomerization and subsequent fibrillization are distinct, and may therefore require equally distinct therapeutic approaches. Prior studies have suggested that amide derivatives of ferulic acid, a natural polyphenol, may combat multiple AD pathologies, though its impact on Aβ aggregation is controversial. We designed and synthesized a systematic library of amide derivatives of ferulic acid and evaluated their anti-oligomeric and anti-fibrillary capacities independently. Azetidine tethered, triphenyl derivatives were the most potent anti-oligomeric agents (compound 2i: IC50 = 1.8 μM ± 0.73 μM); notably these were only modest anti-fibrillary agents (20.57% inhibition of fibrillization), and exemplify the poor correlation between anti-oligomeric/fibrillary activities. These data were subsequently codified in an in silico QSAR model, which yielded a strong predictive model of anti-Aβ oligomeric activity (κ = 0.919 for test set; κ = 0.737 for validation set).
Carbonyl azetidine substituted coumarin fluorescent dye as well as synthesis method and application thereof
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Paragraph 0065-0069, (2021/06/12)
The invention provides a novel carbonyl azetidine substituted coumarin fluorescent dye as well as synthesis and application thereof. The structural innovation of the dye is that carbonyl azetidine is covalently linked to the No.7 site of a coumarin parent. The novel fluorescent dye has excellent fluorescence intensity and light stability, so that the novel fluorescent dye has wide application prospects in the fields of fluorescence detection, fluorescence imaging and the like, especially in the emerging fields of single molecule detection, super-resolution fluorescence imaging and the like. R1 is C1-4 alkyl, and R2 is shown in the specification, X1 is H or C1-2 alkyl, X2 is C1-2 alkyl or shown in the specification, X3 is C1-2 alkyl or shown in the specification, and X4 is C1-2 alkyl.
CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF
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Paragraph 0085; 0086, (2019/04/05)
Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
