Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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Wu J, Tian Y, Wang S, Pistolozzi M, Jin Y, Zhou T, Roy G, Xu L, Tan W
Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
Eur J Med Chem. 2017 Jan 27;126:61-71. doi: 10.1016/j.ejmech.2016.08.061. Epub 2016 Aug 26.
- PubMed ID
- 27744187 [ View in PubMed]
- Abstract
An increase activity of butyrylcholinesterase is believed to contribute to Alzheimer's disease. Bambuterol is a known potent inhibitor of butyrylcholinesterase, but it has undesired cardiac effects and less lipophilicity. Thirteen bambuterol analogues were synthesized using 1-(3, 5-dihydroxyphenyl) ethanone as a starting material. In-vitro cholinesterase assay established that the majority of the compounds are specific butyrylcholinesterase inhibitors. Out of the 13 compounds, two bambuterol derivatives, BD-6 and BD-11 exhibited similar efficacies in inhibiting butyrylcholinesterase with fewer effects on heart and enhanced possibilities of permeating through the blood-brain barrier as compared to bambuterol. These bambuterol analogues may provide better alternatives for treatments of Alzheimer's disease.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Bambuterol Cholinesterase Protein Humans UnknownInhibitorDetails