0000000000430807

AUTHOR

B. Refouvelet

showing 2 related works from this author

(±)- BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3β Inhibition with Calcium Channe…

2021

Multitarget-directed ligands (MTDLs) are considered a promising therapeutic strategy to address the multifactorial nature of Alzheimer's disease (AD). Novel MTDLs have been designed as inhibitors of human acetylcholinesterases/butyrylcholinesterases, monoamine oxidase A/B, and glycogen synthase kinase 3β and as calcium channel antagonists via the Biginelli multicomponent reaction. Among these MTDLs, (±)-BIGI-3h was identified as a promising new hit compound showing in vitro balanced activities toward the aforementioned recognized AD targets. Additional in vitro studies demonstrated antioxidant effects and brain penetration, along with the ability to inhibit the aggregation of both τ protein…

cholinesterasePhysiologyMonoamine oxidaseCognitive NeuroscienceLigandPharmacologyLigandsCalcium ChannelBiochemistry03 medical and health sciences0302 clinical medicineAlzheimer DiseaseIn vivoGSK-3HumansCholinesterasesCholinesterase InhibitorBiginelli reactionAlzheimer's disease; Biginelli reaction; calcium channel; cholinesterases; GSK 3β; MAO; Calcium Channel Blockers; Calcium Channels; Cholinesterase Inhibitors; Glycogen Synthase Kinase 3 beta; Humans; Ligands; Monoamine Oxidase; Alzheimer DiseaseMonoamine OxidaseGSK3B030304 developmental biologyCholinesterase0303 health sciencesGlycogen Synthase Kinase 3 betaVoltage-dependent calcium channelbiologyChemistryCalcium channelCell BiologyGeneral MedicineAlzheimer's diseaseCalcium Channel BlockersCalcium channel GSK 3β MAOMAObiology.proteinCalcium ChannelsCholinesterase InhibitorsGSK 3βMonoamine oxidase ACalcium Channel BlockerAlzheimer’s disease030217 neurology & neurosurgeryHuman
researchProduct

CCDC 650418: Experimental Crystal Structure Determination

2003

Related Article: Y.Jacquot, B.Refouvelet, O.Blacque, M.M.Kubicki, A.Xicluna|2001|C.R.Acad.Sci.,Ser.IIc:Chim.|4|375|doi:10.1016/S1387-1609(01)01243-9

meso-bis(2H-Chromen-2-yl) etherSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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