| Title : Novel cinnamic acid-tryptamine hybrids as potent butyrylcholinesterase inhibitors: Synthesis, biological evaluation, and docking study - Ghafary_2018_Arch.Pharm.(Weinheim)_351_e1800115 |
| Author(s) : Ghafary S , Najafi Z , Mohammadi-Khanaposhtani M , Nadri H , Edraki N , Ayashi N , Larijani B , Amini M , Mahdavi M |
| Ref : Arch Pharm (Weinheim) , 351 :e1800115 , 2018 |
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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 muM. This compound showed a 14-fold higher inhibitory potency than the standard drug donepezil (IC50 = 7.79 +/- 0.81 muM) 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 beta-secretase, which exhibited low activity (inhibition percentage: 38%). |
| PubMedSearch : Ghafary_2018_Arch.Pharm.(Weinheim)_351_e1800115 |
| PubMedID: 30284339 |
Ghafary S, Najafi Z, Mohammadi-Khanaposhtani M, Nadri H, Edraki N, Ayashi N, Larijani B, Amini M, Mahdavi M (2018)
Novel cinnamic acid-tryptamine hybrids as potent butyrylcholinesterase inhibitors: Synthesis, biological evaluation, and docking study
Arch Pharm (Weinheim)
351 :e1800115
Ghafary S, Najafi Z, Mohammadi-Khanaposhtani M, Nadri H, Edraki N, Ayashi N, Larijani B, Amini M, Mahdavi M (2018)
Arch Pharm (Weinheim)
351 :e1800115