Abstract
The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12 ± 0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Acetylcholinesterase / metabolism*
-
Aza Compounds / chemical synthesis
-
Aza Compounds / chemistry
-
Aza Compounds / pharmacology*
-
Cholinesterase Inhibitors / chemical synthesis
-
Cholinesterase Inhibitors / chemistry
-
Cholinesterase Inhibitors / pharmacology*
-
Cyclopentanes / chemical synthesis
-
Cyclopentanes / chemistry
-
Cyclopentanes / pharmacology*
-
Dose-Response Relationship, Drug
-
Drug Evaluation, Preclinical*
-
Models, Molecular
-
Molecular Structure
-
Piperidines / chemistry*
-
Structure-Activity Relationship
Substances
-
Aza Compounds
-
Cholinesterase Inhibitors
-
Cyclopentanes
-
Piperidines
-
piperidine
-
Acetylcholinesterase