Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors

Medicinal Chemistry Research
2013.0

Abstract

New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimer's disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of thienopyridine analogs of tacrine were synthesized and investigated for their ability to inhibit the activity of AChE in comparison with tacrine. All the compounds were found to inhibit AChE activity, especially compounds 7b and 11a, which were found to be more potent than tacrine.

Knowledge Graph

Similar Paper

Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors
Medicinal Chemistry Research 2013.0
Syntheses of coumarin–tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase
Bioorganic & Medicinal Chemistry 2014.0
Pyrano[3,2-c]quinoline−6-Chlorotacrine Hybrids as a Novel Family of Acetylcholinesterase- and β-Amyloid-Directed Anti-Alzheimer Compounds
Journal of Medicinal Chemistry 2009.0
Design, Synthesis, and Biological Evaluation of Dual Binding Site Acetylcholinesterase Inhibitors:  New Disease-Modifying Agents for Alzheimer's Disease
Journal of Medicinal Chemistry 2005.0
Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment
Bioorganic & Medicinal Chemistry Letters 2019.0
Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer’s disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids
Bioorganic & Medicinal Chemistry Letters 2019.0
Hybrids of oxoisoaporphine-tacrine congeners: Novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors
European Journal of Medicinal Chemistry 2011.0
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease
Bioorganic & Medicinal Chemistry Letters 2010.0
Design, synthesis and biological evaluation of novel indano- and thiaindano-pyrazoles with potential interest for Alzheimer's disease
MedChemComm 2013.0
Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer’s disease
Bioorganic & Medicinal Chemistry Letters 2013.0