77474-23-8Relevant 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
, 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.
Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335)
Llinàs-Brunet, Montse,Bailey, Murray D.,Goudreau, Nathalie,Bhardwaj, Punit K.,Bordeleau, Josée,B?s, Michael,Bousquet, Yves,Cordingley, Michael G.,Duan, Jiamin,Forgione, Pat,Garneau, Michel,Ghiro, Elise,Gorys, Vida,Goulet, Sylvie,Halmos, Ted,Kawai, Stephen H.,Naud, Julie,Poupart, Marc-André,White, Peter W.
experimental part, p. 6466 - 6476 (2010/11/04)
C-Terminal carboxylic acid containing inhibitors of the NS3 protease are reported. A novel series of linear tripeptide inhibitors that are very potent and selective against the NS3 protease are described. A substantial contribution to the potency of these
2-AMINOCARBONYL-QUINOLINE COMPOUNDS AS PLATELET ADENOSINE DIPHOSPHATE RECEPTOR ANTAGONISTS
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Page 42, (2010/02/07)
Compounds of formula (I), where m, n, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.