STRUCTURE-ACTIVITY RELATIONS IN ORGANOPHOSPHORUS INHIBITED ACETYLCHOLINESTERASE REACTIVATORS .I. METHIODIDES OF NEW MONOAND 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 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. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company