D.V. Kalinin, V.I. Pantsurkin, B.Ya. Syropyatov, I.P. Rudakova, Yu L. Danilov, M.I. Vahrin

To find compounds with great surface anesthetic activity eleven substances (five toluidides, one anilide and five mesidides of N-alkylpyrrolidine-2-carboxylic acid) were synthesized by known method. These compounds were investigated on rabbit cornea by method of Rainier. Acute toxicity was studied on white mice by intravenous administration. Compounds with higher surface anesthetic activity than commonly used drugs (lidocaine, ropivacaine) were detected. It was found that with increasing lipophilicity of the substituent at the pyrrolidine nitrogen atom increases the duration of surface anesthetic action and acute toxicity of the substance. The transition from toluidides to mesidides of N-alkylpyrrolidine-2-carboxylic acid contributes to the manifestation of surface anesthetic activity.