(2018) Novel cinnamic acid–tryptamine hybrids as potent butyrylcholinesterase inhibitors: Synthesis, biological evaluation, and docking study. Archiv der Pharmazie. ISSN 03656233 (ISSN)
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Abstract
A novel series of cinnamic acid–tryptamine hybrids was designed, synthesized, and evaluated as cholinesterase inhibitors. Anticholinesterase assays showed that all of the synthesized compounds displayed a clearly selective inhibition of butyrylcholinesterase (BChE), but only a moderate inhibitory effect toward acetylcholinesterase (AChE) was detected. Among these cinnamic acid–tryptamine hybrids, compound 7d was found to be the most potent inhibitor of BChE with an IC50 value of 0.55 ± 0.04 μM. This compound showed a 14-fold higher inhibitory potency than the standard drug donepezil (IC50 = 7.79 ± 0.81 μM) and inhibited BChE through a mixed-type inhibition mode. Moreover, a docking study revealed that compound 7d binds to both the catalytic anionic site (CAS) and the peripheral anionic site (PAS) of BChE. Also, compound 7d was evaluated against β-secretase, which exhibited low activity (inhibition percentage: 38). © 2018 Deutsche Pharmazeutische Gesellschaft
| Item Type: | Article |
|---|---|
| Keywords: | Alzheimer's disease butyrylcholinesterase inhibitors cholinesterase inhibition cinnamic acid docking study tryptamine Acetylcholinesterase Animals Butyrylcholinesterase Cholinesterase Inhibitors Cinnamates Dose-Response Relationship, Drug Eels Horses Kinetics Molecular Docking Simulation Molecular Structure Neuroprotective Agents PC12 Cells Rats Structure-Activity Relationship Tryptamines cholinesterase cholinesterase inhibitor cinnamic acid derivative neuroprotective agent tryptamine derivative animal chemical structure chemistry dose response eel horse metabolism molecular docking PC12 cell line rat structure activity relation synthesis |
| Journal or Publication Title: | Archiv der Pharmazie |
| Volume: | 351 |
| Number: | 10 |
| Identification Number: | https://doi.org/10.1002/ardp.201800115 |
| ISSN: | 03656233 (ISSN) |
| Depositing User: | Mr mahdi sharifi |
| URI: | http://eprints.ssu.ac.ir/id/eprint/32062 |
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