LMP2 Inhibitors as a Potential Treatment for Alzheimer’s Disease was written by Bhattarai, Deepak;Lee, Min Jae;Baek, Ahruem;Yeo, In Jun;Miller, Zachary;Baek, Yu Mi;Lee, Sukyeong;Kim, Dong-Eun;Hong, Jin Tae;Kim, Kyung Bo. And the article was included in Journal of Medicinal Chemistry in 2020.Application of 87694-53-9 This article mentions the following:
The immunoproteasome (iP), an inducible proteasome variant harboring three immunosubunits, low mol. mass polypeptide-2 (LMP2), multicatalytic endopeptidase complex subunit-1, and low mol. mass polypeptide-7 (LMP7), is involved in multiple facets of inflammatory responses. We recently reported that YU102, a dual inhibitor of the iP subunit LMP2 and the constitutive proteasome catalytic subunit β1, ameliorates cognitive impairments in mouse models of Alzheimer’s disease (AD) independently of amyloid deposits. To investigate whether inhibition of LMP2 is sufficient to improve the cognitive functions of AD mice, here we prepared 37 YU102 analogs and identified a potent LMP2 inhibitor DB-310 (28) (IC50: 80.6 nM) with improved selectivity and permeability in cells overexpressing ABCB1 transporters. We show that DB-310 induces suppression of IL-1α production in microglia cells and improves cognitive functions in the Tg2576 transgenic mouse model of AD. This study supports that inhibition of LMP2 is a promising therapeutic strategy for treatment of AD. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Application of 87694-53-9).
(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Application of 87694-53-9
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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics