[Study on reversible anticholinesterase agents: synthesis of derivatives of 1,3,2-dioxaphosphorinane 2-oxide].

Paper

[Study on reversible anticholinesterase agents: synthesis of derivatives of 1,3,2-dioxaphosphorinane 2-oxide].

Published Nov 1, 1987 · Cui Ta, Ding Zk

Acta pharmaceutica Sinica

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Abstract

In order to search for more effective reversible antieholinesterase agents, a series of substituted 1, 3, 2-dioxaphosphorinane 2-xride were synthesized. In preliminary pharmacological test in mice, most of the compounds showed anticholinesterase activity, of which Ⅲ_2, Ⅲ_(10) and Ⅲ_(12) were more potential than the "leading compound" Ⅲ_1. All compounds were synthesized by condensation of the corresponding hydroxyor amino-compounds with 2-chloro-1, 3, 2-dioxaphosphorinane 2-oxide. The latter was obtained from the cyclization of phosphorus oxychloride with 1, 3-propanediol. In the mass spectra of compounds Ⅱ, we found the general occurrence of McLafferty rearrangement. By means of high resolution mass spectra analysis and metastable ion determination, the possible mechanism was confirmed.

Study Snapshot

Substituted 1,3,2-dioxaphosphorinane 2-xride compounds show potential as reversible anticholinesterase agents, with III_2, III_(10), and III_(12) showing more potential than the leading compound III_1.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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