Synthesis of aldoxime analogs of arecoline as reactivators of organophosphorus inhibited cholinesterase

J. N. Wells, J. N. Davisson, I. Boime, D. R. Haubrich, G. K.W. Yim

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Abstract

A series of arecoline‐like aldoximes were synthesized and evaluated as potential reactivators of organophosphate‐inhibited cholinesterase. These arecoline analogs were patterned after the potent quaternary oximes 2‐PAM and TMB‐4 and were synthesized by sodium borohydride reduction of the corresponding pyridinium aldoxime. Biological results show that although these aldoximes are less toxic than the quaternary aldoximes, they are much less effective as reactivators. They did exhibit weak muscarinic activity (1/60 that of arecoline) on dog blood pressure and guinea pig ileum.

Original languageEnglish
Pages (from-to)1190-1192
Number of pages3
JournalJournal of Pharmaceutical Sciences
Volume56
Issue number9
DOIs
StatePublished - Sep 1967

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