Synthesis of Some Phenylisoindoline-1,3-Diones and their Acetylcholinesterase and Butyryl Cholinesterase Inhibitory Activities
F. O. Taiwo *
Department of Chemistry, Obafemi Awolowo University, Nigeria.
C. A. Obafemi
Department of Chemistry, Obafemi Awolowo University, Nigeria.
E. M. Obuotor
Department of Biochemistry and Molecular Biology, Obafemi Awolowo University, Nigeria.
I. J. Olawuni
Department of Biochemistry and Molecular Biology, Obafemi Awolowo University, Nigeria.
*Author to whom correspondence should be addressed.
Abstract
Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties.
Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The acetylcholinesterase and butyryl cholinesterase inhibitions were determined by Spectro photochemical analysis of acetylthiocholine and butyryl choline chloride.
Results: Compounds 6 (IC50 = 30±3 µg/mL) and 4 (IC50 = 141±60 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 4 (IC50 = 102±10 µg/mL), 5 (IC50 = 105 ± 20 µg/mL) and 2 (IC50 = 190 ± 10 µg/mL), were found to be most active inhibitor against butyryl cholinesterase.
Conclusion: The considerable acetylcholinesterase and butyryl cholinesterase inhibitory activities of the synthesized compounds makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.
Keywords: Alzheimer's disease, acetylcholine, acetylcholinesterase, butyryl cholinesterase, serine, chalcones