77474-14-7Relevant articles and documents
Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease
Estrada Valencia, Martín,Herrera-Arozamena, Clara,de Andrés, Lucía,Pérez, Concepción,Morales-García, José A.,Pérez-Castillo, Ana,Ramos, Eva,Romero, Alejandro,Vi?a, Dolores,Yá?ez, Matilde,Laurini, Erik,Pricl, Sabrina,Rodríguez-Franco, María Isabel
supporting information, p. 534 - 553 (2018/07/25)
In this work we describe neurogenic and neuroprotective donepezil-flavonoid hybrids (DFHs), exhibiting nanomolar affinities for the sigma-1 receptor (σ1R) and inhibition of key enzymes in Alzheimer's disease (AD), such as acetylcholinesterase (AChE), 5-lipoxygenase (5-LOX), and monoamine oxidases (MAOs). In general, new compounds scavenge free radical species, are predicted to be brain-permeable, and protect neuronal cells against mitochondrial oxidative stress. N-(2-(1-Benzylpiperidin-4-yl)ethyl)-6,7-dimethoxy-4-oxo-4H-chromene-2-carboxamide (18) is highlighted due to its interesting biological profile in σ1R, AChE, 5-LOX, MAO-A and MAO-B. In phenotypic assays, it protects a neuronal cell line against mitochondrial oxidative stress and promotes maturation of neural stem cells into a neuronal phenotype, which could contribute to the reparation of neuronal tissues. Molecular modelling studies of 18 in AChE, 5-LOX and σ1R revealed the main interactions with these proteins, which will be further exploited in the optimization of new, more efficient DFHs.
Synthesis of 2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-ol; A quinoline building block for simeprevir synthesis
Rádl, Stanislav,Rezková, Hana,Obadalová, Iva,Srbek, Jan,B?ichá?, Ji?í,Pekárek, Tomá?
, p. 899 - 908 (2014/04/03)
Two synthetic approaches to the achiral quinoline fragment of simeprevir are described. Both approaches are based on the synthesis of methyl 4-hydroxy-7-methoxy-8-methylquinoline-2-carboxylate, protection of its 4-hydroxyl group, and construction of the thiazole ring from the ester group at the 2-position. The last step is acid deprotection of the 4-hydroxyl protecting group. Georg Thieme Verlag Stuttgart. New York.
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
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Page/Page column 30-31, (2010/02/14)
The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.