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J Enzyme Inhib Med Chem ; 34(1): 631-637, 2019 Dec.
Article in English | MEDLINE | ID: mdl-30727776

ABSTRACT

A series of 3-substituted-7-aminoalcoxy-coumarin was designed and evaluated as cholinesterase inhibitors and antioxidants. All compounds were effective in inhibiting AChE with potencies in the nanomolar range. The 3-(4-(dimethylamino)phenyl)-7-aminoethoxy-coumarin (6a) was considered a hit, showing good AChE inhibition potency (IC50 = 20 nM) and selectivity (IC50 BuChE/AChE = 354), quite similar to the reference drug donepezil (IC50 = 6 nM; IC50 BuChE/AChE = 365), also presenting antioxidant properties, low citotoxicity and good-predicted ADMET properties. The mode of action (mixed-type) and SAR analysis for this series of compounds were described by means of kinetic and molecular modeling evaluations.


Subject(s)
Acetylcholinesterase/metabolism , Antioxidants/pharmacology , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/pharmacology , Coumarins/pharmacology , Drug Discovery , Animals , Antioxidants/chemical synthesis , Antioxidants/chemistry , Cell Survival/drug effects , Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/chemistry , Coumarins/chemical synthesis , Coumarins/chemistry , Dose-Response Relationship, Drug , Electrophorus , Horses , Mice , Models, Molecular , Molecular Structure , Structure-Activity Relationship , Tumor Cells, Cultured
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