Chemical Biology & Drug Design · 2015 · 23 citations · 15 references
MedicineMedicinal ChemistryPharmacologyDrug DiscoveryEnzymologyNeuropharmacologyCholinergic PharmacologyCholinergic SignalingEnzyme InhibitionNeurodegenerative Disease PharmacologyNeuroprotectionStructure-activity Relationship AnalysisAcetylcholinesterase InhibitorsAcetylcholinesterase TargetsAche InhibitionPharmacological Treatment Of DementiaTherapeutic Target IdentificationTherapeutic Target Validation
A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).
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