Abstract
Two phosphoric 4-nitroanilides Z2P(O)NH-phi-NO2 (A, Z = Me; B, Z = NMe2) have been prepared and purified by chromatographic techniques. Their spectral data (uv, ir and 1H-nmr) have been determined, and compared with those of other similar compounds. Their ability to inhibit acetylcholinesterase has been measured by a modification of Ellman's method. The data, as computed according to the Michaelis scheme, indicate that A is not an inhibitor, whereas B is a reversible mixed one. These differences are discussed in terms of hydrophobic interactions.
MeSH terms
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Acetylcholinesterase / metabolism
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Anilides / chemical synthesis*
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Anilides / isolation & purification
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Anilides / pharmacology
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Animals
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Cholinesterase Inhibitors / chemical synthesis*
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Chromatography, High Pressure Liquid
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Chromatography, Thin Layer
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Electrophorus
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Indicators and Reagents
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Kinetics
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Magnetic Resonance Spectroscopy
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Organophosphorus Compounds / chemical synthesis*
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Organophosphorus Compounds / isolation & purification
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Organophosphorus Compounds / pharmacology
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Spectrophotometry
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Structure-Activity Relationship
Substances
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Anilides
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Cholinesterase Inhibitors
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Indicators and Reagents
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Organophosphorus Compounds
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N-(4-nitrophenyl)dimethylphosphinamide
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N,N,N',N'-tetramethyl-N''-(4-nitrophenyl)phosphoric triamide
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Acetylcholinesterase