Relationships between the structure of organophosphorus compounds and their activity as acetylcholinesterase inhibitors.

This paper discusses the relation between chemical structure and inactivation of the enzyme acetylcholinesterase (AChE) by organophosphorus esters, in terms of reactivity and steric effects. The discussion is centered in organophosphorus esters of the type (R) (R') P(O) X, where X is a readily displaceable group and R and R' are various combinations of alkyl, alkoxy, alkylthio, and amido moieties. Specific examples illustrating the effect of AChE inhibition on the selective toxicity of organophosphorus esters for insects and mammals are also presented.