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Article

Succinimide Derivatives as Acetylcholinesterase Inhibitors—In Silico and In Vitro Studies

by
Błażej Grodner
1,
Dariusz Maciej Pisklak
2 and
Łukasz Szeleszczuk
2,*
1
Chair and Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Str., 02-097 Warsaw, Poland
2
Department of Organic and Physical Chemistry, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Str., 02-097 Warsaw, Poland
*
Author to whom correspondence should be addressed.
Curr. Issues Mol. Biol. 2024, 46(6), 5117-5130; https://doi.org/10.3390/cimb46060307
Submission received: 24 April 2024 / Revised: 16 May 2024 / Accepted: 21 May 2024 / Published: 22 May 2024
(This article belongs to the Special Issue Synthesis and Theoretical Study of Bioactive Molecules)

Abstract

We studied the effect of succinimide derivatives on acetylcholinesterase activity due to the interest in compounds that influence this enzyme’s activity, which could help treat memory issues more effectively. The following parameters were established for this purpose based on kinetic investigations of the enzyme in the presence of succinimide derivatives: the half-maximal inhibitory concentration, the maximum rate, the inhibition constant, and the Michaelis–Menten constant. Furthermore, computational analyses were performed to determine the energy required for succinimide derivatives to dock with the enzyme’s active site. The outcomes acquired in this manner demonstrated that all compounds inhibited acetylcholinesterase in a competitive manner. The values of the docking energy parameters corroborated the kinetic parameter values, which indicated discernible, albeit slight, variations in the inhibitory intensity among the various derivatives.
Keywords: acetylcholine; acetylcholinesterase; Alzheimer’s disease; competitive inhibitors; enzyme activity; succinimide derivatives acetylcholine; acetylcholinesterase; Alzheimer’s disease; competitive inhibitors; enzyme activity; succinimide derivatives

Share and Cite

MDPI and ACS Style

Grodner, B.; Pisklak, D.M.; Szeleszczuk, Ł. Succinimide Derivatives as Acetylcholinesterase Inhibitors—In Silico and In Vitro Studies. Curr. Issues Mol. Biol. 2024, 46, 5117-5130. https://doi.org/10.3390/cimb46060307

AMA Style

Grodner B, Pisklak DM, Szeleszczuk Ł. Succinimide Derivatives as Acetylcholinesterase Inhibitors—In Silico and In Vitro Studies. Current Issues in Molecular Biology. 2024; 46(6):5117-5130. https://doi.org/10.3390/cimb46060307

Chicago/Turabian Style

Grodner, Błażej, Dariusz Maciej Pisklak, and Łukasz Szeleszczuk. 2024. "Succinimide Derivatives as Acetylcholinesterase Inhibitors—In Silico and In Vitro Studies" Current Issues in Molecular Biology 46, no. 6: 5117-5130. https://doi.org/10.3390/cimb46060307

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