Synthesis and Properties of 2-S-[2'-(N, N-Dialkylamino) ethyl] thio-1, 3, 2-dioxaphosphorinane 2-Oxide and of the Corresponding Quaternary Derivatives as Potential …
…, Y Ashani, Y Grunfeld, A Kalir, S Cohen
文献索引：Amitai; Ashani; Grunfeld; Kalir; Cohen Journal of Medicinal Chemistry, 1976 , vol. 19, # 6 p. 810 - 813
A new series of cyclic organophosphorus esters, 2-S-[2'-(N, N-dialkylaminojethyl] thio-1, 3, 2- dioxaphosphorinane% oxide and their quaternary derivatives, was synthesized and studied as potential antiglaucoma agents. These compounds inhibit acetylcholinesterase (EC 3.1. 1.7) at a bimolecular rate constant (hi) in the range of 10" 104 M min I. Values of the affinity (K) and phosphorylation (k') rate constants for this enzyme indicate that k'is responsible for ...
