Dataset : Three-Component Access to Functionalized Spiropyrrolidine Heterocyclic Scaffolds and Their Cholinesterase Inhibitory Activity

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Quotation

Sarra Boudriga ; Saoussen Haddad ; Vikneswaran Murugaiyah ; Mohedinne Askri ; Michael Knorr ; Carsten Strohmann ; Christopher Golz (2020): Three-Component Access to Functionalized Spiropyrrolidine Heterocyclic Scaffolds and Their Cholinesterase Inhibitory Activity . Multidisciplinary Digital Publishing Institute. doi:10.3390/molecules25081963

General metadata

Identifier : local : FR-18008901306731-2021-03-12 external : doi:10.3390/molecules25081963
Description :
A novel one-pot [3+2]-cycloaddition reaction of (E)-3-arylidene-1-phenyl-succinimides, cyclic 1,2-diketones (isatin, 5-chloro-isatin and acenaphtenequinone), and diverse α-aminoacids such as 2-phenylglycine or sarcosine is reported. The reaction provides succinimide-substituted dispiropyrrolidine derivatives with high regio- and diastereoselectivities under mild reaction conditions. The stereochemistry of these N-heterocycles has been confirmed by four X-ray diffraction studies. Several synthetized compounds show higher inhibition on acetylcholinesterase (AChE) than butyrylcholinesterase (BChE). Of the 17 synthesized compounds tested, five exhibit good AChE inhibition with IC50 of 11.42 to 22.21 µM. A molecular docking study has also been undertaken for compound 4n possessing the most potent AChE inhibitory activity, disclosing its binding to the peripheral anionic site of AChE enzymes.
Discipline :
chemistry, organic (chemistry)
Keywords :

Dates :
Data acquisition : from 2019 to 2020
Data provision : 23 Apr 2020
Metadata record :
Creation : 12 Mar 2021

Update periodicity : no update
Language : English (eng)
Audience : Research

Administrative metadata

Data creatorsAffiliation
Sarra BoudrigaLR11ES39 (TUN)
Saoussen HaddadLR11ES39 (TUN)
Vikneswaran MurugaiyahUSM (MYS)
Mohedinne AskriLR11ES39 (TUN)
Michael KnorrUTINAM (FRA)
Carsten StrohmannTU Dortmund (DEU)
Christopher GolzTU Dortmund (DEU)
Publisher : Multidisciplinary Digital Publishing Institute
Science contact : Michael Knorr website e-mail
Access : available

Technical metadata

Formats : application/pdf
Data acquisition methods :
Datatype : Dataset

Publications

  • Three-Component Access to Functionalized Spiropyrrolidine Heterocyclic Scaffolds and Their Cholinesterase Inhibitory Activity (doi:10.3390/molecules25081963)
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