68898-11-3Relevant academic research and scientific papers
Benzofuranyl-2-imidazoles as imidazoline I2 receptor ligands for Alzheimer's disease
Brocos-Mosquera, Iria,Callado, Luis F.,Daelemans, Dirk,De Jonghe, Steven,Djikic, Teodora,Escolano, Carmen,Loza, M. Isabel,Molins, Elies,Nikolic, Katarina,Radan, Milica,Vasilopoulou, Foteini,Bagán, Andrea,Brea, José,García-Fuster, M. Julia,García-Sevilla, Jesús A.,Gri?án-Ferré, Christian,Hernández-Hernández, Elena,Martínez, Antón L.,Pérez, Belén,Pallàs, Mercè,Rodriguez-Arévalo, Sergio
, (2021/07/28)
Recent findings unveil the pharmacological modulation of imidazoline I2 receptors (I2-IR) as a novel strategy to face unmet medical neurodegenerative diseases. In this work, we report the chemical characterization, three-dimensional quantitative structure-activity relationship (3D-QSAR) and ADMET in silico of a family of benzofuranyl-2-imidazoles that exhibit affinity against human brain I2-IR and most of them have been predicted to be brain permeable. Acute treatment in mice with 2-(2-benzofuranyl)-2-imidazole, known as LSL60101 (garsevil), showed non-warning properties in the ADMET studies and an optimal pharmacokinetic profile. Moreover, LSL60101 induced hypothermia in mice while decreased pro-apoptotic FADD protein in the hippocampus. In vivo studies in the familial Alzheimer's disease 5xFAD murine model with the representative compound, revealed significant decreases in the protein expression levels of antioxidant enzymes superoxide dismutase and glutathione peroxidase in hippocampus. Overall, LSL60101 plays a neuroprotective role by reducing apoptosis and modulating oxidative stress.
Vinylogous Elimination/C-H Functionalization/Allylation Cascade Reaction of Allenoate Adducts: Synthesis of Ring-Fused Dihydropyridinones
Sun, Manman,Chen, Weida,Wu, Haijian,Xia, Xiangyu,Yang, Jianguo,Wang, Lei,Shen, Guodong,Wang, Zhiming
supporting information, p. 8313 - 8319 (2020/11/03)
A palladium-catalyzed cascade reaction of β′-allenoate adducts with aryl/heteroaryl carboxamides through a vinylogous elimination/C-H functionalization/intramolecular allylation reaction sequence has been developed with high Z stereoselectivity. Various ring-fused dihydropyridinones bearing an α,β-unsaturated ester substituent are obtained. It is the first example of application of the allenoate adducts to C-H functionalization annulations as practical precursors of hard-to-get functionalized electron-deficient 1,3-butadienes. Using air as the terminal oxidant also shows a great advantage in environmental friendliness.
BITTER TASTE MODULATORS
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Page/Page column 74, (2012/01/06)
The present invention includes antagonists of human type 2 taste receptors (hT2Rs) having structural Formula (I). The present invention also provides compositions containing these antagonists, the use of these antagonists for modulating taste perception, particularly bitter taste, and the method of preparing these antagonists (I).
N -(3-Fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl) arylcarboxamides as selective dopamine D3 receptor ligands: Critical role of the carboxamide linker for d3 receptor selectivity
Banala, Ashwini K.,Levy, Benjamin A.,Khatri, Sameer S.,Furman, Cheryse A.,Roof, Rebecca A.,Mishra, Yogesh,Griffin, Suzy A.,Sibley, David R.,Luedtke, Robert R.,Newman, Amy Hauck
experimental part, p. 3581 - 3594 (2011/07/29)
N-(3-Fluoro-4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazine-1-yl)butyl) arylcarboxamides were prepared and evaluated for binding and function at dopamine D3 receptors (D3Rs) and dopamine D2 receptors (D2Rs). In this series, we discovered some of the mos
