Antiradical Activity of Some Antiulcer and Local-Anaesthetic Active Substances

Overview

The free radical scavenging effect of the hydrochloride of (±)-trans-2-(1-pyrrolidinyl-) cyclohexylesterof 3-(n)-pentyloxy carbanilic acid, pentacaine (trapencaine I.N.N), and its derivatives and othersubstances, lidocaine, stobadine, mannitol, and ascorbic acid was tested in the presence of diphenyl-p-picrylhydrazyl (decrease in absorbance). In this method, more pronounced antiradical activitywas observed with trapencaine, more effective than stobadine, ascorbate, and mannitol. Trapen-caine derivatives and lidocaine were less effective in comparison with trapencaine. After introducinga 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 thetransisomer. 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