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Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors
- Source :
- European Journal of Medicinal Chemistry. 43:657-661
- Publication Year :
- 2008
- Publisher :
- Elsevier BV, 2008.
-
Abstract
- The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as potential acetylcholinesterase and butyrylcholinesterase inhibitors by means of a chemiluminescent microassay. Although most of the new compounds did not show significant cholinesterase inhibition potency, three of them displayed selective antiacetylcholinesterase activity in the micromolar range.
- Subjects :
- Alkylation
ANTIBUTYRYLCHOLINESTERASE ACTIVITY
Acylation
IMIDAZO[2
Chemical synthesis
Inhibitory Concentration 50
chemistry.chemical_compound
Drug Discovery
Animals
Thiazole
Butyrylcholinesterase
Cholinesterase
Pharmacology
chemistry.chemical_classification
Binding Sites
Dose-Response Relationship, Drug
biology
Organic Chemistry
Imidazoles
Benzene
Biological activity
General Medicine
Acetylcholinesterase
CHEMILUMINESCENCE
Kinetics
Thiazoles
Enzyme
ANTIACETYLCHOLINESTERASE ACTIVITY
chemistry
Biochemistry
Enzyme inhibitor
Drug Design
Luminescent Measurements
biology.protein
Cholinesterase Inhibitors
1-B]THIAZOLE
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 43
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....83ef0c75fbb6878843a3935b6f83810c