A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). The assessment of IC50 values revealed 1 as a weak inhibitor of both tested enzymes.
- MeSH
- Acridines chemical synthesis chemistry pharmacology MeSH
- Alzheimer Disease drug therapy enzymology MeSH
- Butyrylcholinesterase chemistry pharmacology MeSH
- Cholinesterase Inhibitors chemical synthesis chemistry pharmacology MeSH
- Cholinesterases chemistry MeSH
- Heterocyclic Compounds, 3-Ring chemical synthesis chemistry pharmacology MeSH
- Humans MeSH
- Drug Evaluation, Preclinical MeSH
- Tacrine chemistry pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH