Design, synthesis, and evaluation of 3,7-substituted coumarin derivatives as multifunctional Alzheimer’s disease agents
Sheunopa C. Mzezewa, Sylvester I. Omoruyi, Luke S. Zondagh, Sarel F. Malan, Okobi E. Ekpo, Jacques Joubert
Abstract
-compromised SH-SY5Y neuroblastoma cells were also observed, with no inherent cytotoxicity at 10 µM for all compounds. The overall results demonstrated that substitution of the phenylethyloxy moiety at the 7-position imparted superior general activity to the derivatives, with the propargylamine substitution at the 3-position, in particular, displaying the best MAO-B selectivity and neuroprotection.
Topics & Concepts
CoumarinNeuroprotectionCytotoxicityChemistryCholinesteraseMonoamine oxidaseSelectivityMoietyMonoamine oxidase BAcetylcholinesteraseEnzymePharmacologySelegilineStereochemistryBiochemistryCombinatorial chemistryIn vitroOrganic chemistryMedicineDiseaseInternal medicineParkinson's diseaseCatalysisCholinesterase and Neurodegenerative DiseasesComputational Drug Discovery MethodsMedicinal Plants and Neuroprotection