Journal of Medicinal Chemistry · 2014 · 65 citations · 35 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryNeuropharmacologyChemical Library DesignCholinergic PharmacologyEnzyme InhibitionLead Compound DesignPotency OptimizationStructure-activity Relationship AnalysisChemical Synthesis Of AnaloguesIndole ChemistryIndole DerivativesIndole SynthesisMedicinal Chemistry ApplicationsMonoamine Oxidase Inhibitor InteractionsMonoamine Oxidase InhibitorsSerotonergic Drug Discovery
On the basis of N-((5-(3-(1-benzylpiperidin-4-yl)propoxy)-1-methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (II, ASS234) and QSAR predictions, in this work we have designed, synthesized, and evaluated a number of new indole derivatives from which we have identified N-methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine (2, MBA236) as a new cholinesterase and monoamine oxidase dual inhibitor.
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A new and rapid colorimetric determination of acetylcholinesterase activity
George L. Ellman, K. Diane Courtney, Valentino Andres et al. · Biochemical Pharmacology · 1961 · 26.9K citations