Structure-Activity Relations in Organophosphorus Inhibited Acetylcholinesterase Reactivators I: Methiodides of New Mono-and Dioximes with Pyridine Nucleus

A series of methiodides deriving from syn β-pyridyl-α,-β-dihydroxyimino-propioanilides, from β-pyridyl-β-oxo-α-hydroxyimino-propioanilides showing the hydroxyimino group in the two possible configurations and from anti β-pyridyl-β-hydroxyimino-propioanilides was prepared. The in vitro acetylcholines...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1969-04, Vol.58 (4), p.460-464
Main Authors: Grifantini, Mario, Martelli, Sante, Stein, Maria L.
Format: Article
Language:English
Subjects:
Acetylcholinesterase reactivators-organo-phosphorus inhibited
Cholinesterase Inhibitors
Infrared Rays
IR spectrophotometry-structure
Isoflurophate - pharmacology
Methiodides of mono- and dioximes-synthesis
Oximes - chemical synthesis
Oximes - pharmacology
Pyridines - chemical synthesis
Pyridines - pharmacology
Spectrophotometry
Structure-activity relationships-acetylcholinesterase re-activators
Ultraviolet Rays
UV spectrophotometer-structure
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Summary:A series of methiodides deriving from syn β-pyridyl-α,-β-dihydroxyimino-propioanilides, from β-pyridyl-β-oxo-α-hydroxyimino-propioanilides showing the hydroxyimino group in the two possible configurations and from anti β-pyridyl-β-hydroxyimino-propioanilides was prepared. The in vitro acetylcholinesterase-reactivating activity of the new compounds was evaluated. The results show that the β-hydroxyimino group contributes very little to the reactivation, probably because it is held by the amide group through a hydrogen bond; in fact, the β-monoximes are nearly inactive. Therefore the activity of the dioximes should be ascribed to the α-hydroxyimino group.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600580415