Summary:
The free radical scavenging effect of the hydrochloride of (±)-trans-2-(1-pyrrolidinyl-) cyclohexylester
of 3-(n)-pentyloxy carbanilic acid, pentacaine (trapencaine I.N.N), and its derivatives and other
substances, lidocaine, stobadine, mannitol, and ascorbic acid was tested in the presence of diphenyl-p-picrylhydrazyl (decrease in absorbance). In this method, more pronounced antiradical activity
was observed with trapencaine, more effective than stobadine, ascorbate, and mannitol. Trapen-
caine derivatives and lidocaine were less effective in comparison with trapencaine. After introducing
a methylene group into the hydrophilic moiety of the trapencaine molecule (stereoisomers P-18,
P-20), there was a loss of antiradical activity, but the cis-isomer is more effective than the
transisomer. The results demonstrate the existence of relationships between the chemical structure,
antiradical and gastric-cytoprotective activity.
Key words:
trapencaine - lidocaine - stobadine - antiradical activity
- gastrocytoprotective activity
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