Sulfonamide Derivatives of 2-Amino-1-phenylethane as Suitable Cholinesterase Inhibitors
Purpose: To evaluate the enzyme inhibition activity of N-substituted sulfamoyl derivatives of 2-amino-1- phenylethane as probable new drug candidates for the treatment of Alzheimer's diseases. Methods: A series of sulfamoyl derivatives, 3a-l, of 1-amino-2-phenylethane (1) were synthesized by re...
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Veröffentlicht in: | Tropical journal of pharmaceutical research 2014-09, Vol.13 (5), p.739 |
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Sprache: | eng |
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Zusammenfassung: | Purpose: To evaluate the enzyme inhibition activity of N-substituted
sulfamoyl derivatives of 2-amino-1- phenylethane as probable new drug
candidates for the treatment of Alzheimer's diseases. Methods: A
series of sulfamoyl derivatives, 3a-l, of 1-amino-2-phenylethane (1)
were synthesized by reacting with various aryl sulfonyl chlorides,
2a-l, in the presence of aqueous Na2CO3 solution under definite pH
control. All the synthesized molecules were screened against three
enzymes, acetyl cholinesterase (AChE), butyryl cholinesterase (BChE)
and lipoxygenase (LOX). The synthesized derivatives were further
characterized by infra-red spectroscopy (IR), nuclear magnetic
resonance (1H- NMR) and electron ionization-mass spectrometry
(EI-MS) for structure elucidation. Results: Screening against acetyl
cholinesterase (AChE), butyryl cholinesterase (BChE) and lipoxygenase
(LOX) showed these molecules to be suitable inhibitors of
cholinesterase enzymes, AChE and BChE, relative to eserine, the
reference standard. The molecule, 3c, remained effective with 50 %
inhibitory concentration (IC50) value of 82.93 ± 0.15 μM
(relative to eserine with IC50 value of 0.04 ± 0.0001 μM)
against AChE; similarly 3d was active against BChE with IC50 value of
45.65 ± 0.48 μM compared to eserine with IC50 value of 0.85
± 0.00 μM. The molecule, 3f, was inactive against all the
three enzymes. Conclusion: Overall, the results indicate that these
compounds are active against cholinesterase enzymes but less potent
against lipoxygenase enzyme. |
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ISSN: | 1596-5996 1596-9827 |
DOI: | 10.4314/tjpr.v13i5.13 |