- Synthesis and characterization of copper-specific tetradendate ligands as potential treatment for Alzheimer's disease
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To regulate copper homeostasis for the therapy of Alzheimer's disease, a series of “tetradendate monoquinoline” (TDMQ) ligands consisting of an 8-aminoquinoline nucleus with a bidentate amine side chain attached at the C2 position of the quinoline moiety, both parts being able to take part in copper chelation, were designed. These TDMQ ligands are potentially able to provide the square planar tetradentate coordination sphere, which is preferred for the extraction of copper(II) from amyloids, with a lower as possible molecular weight, to optimize the passage through different physiological barriers.
- Zhang, Weixin,Huang, Meijie,Bijani, Christian,Liu, Yan,Robert, Anne,Meunier, Bernard
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- Cooperative Lewis Acid Catalysis for the Enantioselective C(sp3)-H Bond Functionalizations of 2-Alkyl Azaarenes
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Herein, we describe the enantioselective C(sp3)-H bond functionalizations of 2-alkyl azaarenes using a cooperative dual Lewis acid catalysis. An achiral Lewis acid activates the unactivated azaarene partner without the need for a strong base. Orthogonally, a chiral-at-metal Lewis acid catalyst enables LUMO lowering and induces chirality. This method tolerates a range of complex molecular scaffolds and exhibits good to excellent yields and selectivity while accepting a wide variety of functional groups.
- Rai, Pramod,Waiba, Satyadeep,Maji, Kakoli,Sahoo, Dibyaranjan,Maji, Biplab
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supporting information
p. 8888 - 8893
(2021/11/24)
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- Preparation of Tetradentate Copper Chelators as Potential Anti-Alzheimer Agents
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The uncontrolled redox activity of metal ions, especially copper, in the brains of patients with Alzheimer's disease (AD) should be considered the origin of intense oxidative damage to neurons in the AD brain. To obtain low-molecular-weight copper chelators that act as tetradentate ligands, we designed new compounds based on an 8-aminoquinoline motif with a lateral chain attached at the 2-position of the aromatic ring. Some of these new ligands, termed TDMQ for TetraDentate MonoQuinolines, are specific for copper chelation. Full characterization of these ligands is reported, as well as their affinities for CuII, and their capacities to inhibit oxidative stress induced by copper–amyloids activated by a reductant. Such metal ligands can be considered as potential anti-AD agents, as they should be able to regulate the homeostasis of copper in brain tissue.
- Zhang, Weixin,Huang, Daya,Huang, Meijie,Huang, Ju,Wang, Dean,Liu, Xingguo,Nguyen, Michel,Vendier, Laure,Mazères, Serge,Robert, Anne,Liu, Yan,Meunier, Bernard
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p. 684 - 704
(2018/02/28)
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- Four-tooth chelating single quinoline derivative, preparation method thereof and application as metal ion regulator for neurodegenerative disease
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The invention provides a four-tooth chelating single quinoline derivative. A structural formula of the derivative is shown as a formula (I) in the description. The derivative provided by the invention can specifically chelate redox active metal ions related to neurodegenerative disease (alzheimer disease, Parkinson disease and amyotrophic lateral sclerosis) metabolic disturbance or copper accumulation disease (Wilson disease), such as copper ion; a complex constant of the derivative to zinc ion is 6 to 12 orders of magnitude lower than that to the copper ion, and the derivative shows stronger anti-oxidative-stress capability; the derivative is simple in preparation method, and has potential application prospect when serving as drugs for treating neurodegenerative disease and drugs for treating copper ion turbulence.
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Paragraph 0055; 0056; 0057
(2018/02/03)
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- 3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors
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Investigation of halogen substitution in lead compound 1 has led to the identification of analogues which combine high affinity for 5-HT1A receptors and potent serotonin reuptake inhibitory activity. Several compounds show an improved selectivity over 5-HT1B and 5-HT1D receptors and a superior pharmacokinetic profile in the rat.
- Lovell, Peter J.,Blaney, Frank E.,Goodacre, Caroline J.,Scott, Claire M.,Smith, Paul W.,Starr, Kathryn R.,Thewlis, Kevin M.,Vong, Antonio K.K.,Ward, Simon E.,Watson, Jeannette M.
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p. 1033 - 1036
(2007/10/03)
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