ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Study of Local Anaesthetics, Part 156: Some Physicochemical and Lipophilic Properties of Pyrrolidinoethyl Esters of o-, m-, p-Alkoxy-Substituted Phenylcarbamic Acid

L. Gyurösiová, E. Sedlárová, and J. Čižmárik

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, SK-832 32 Bratislava

E-mail: sedlarova@fpharm.uniba.sk

Received: 25 October 2001

Abstract: In the series of pyrrolidinoethyl esters of o-, m-, p-alkoxy-substituted phenylcarbamic acid the values of lipophilic parameters (R_M, log P_app, log k) increase with lengthening of alkoxy chain on benzene ring, each methylene group increases the lipophilicity. Comparing advantages and disadvantages of different methods for a drug’s lipophilicity determination, as well as experiences from the laboratory, the easiest and best method seems to be HPLC. According to the results, the highest local anaesthetic activity can be assumed by the compounds with 6—8 carbon atoms in the side chain.

Full paper in Portable Document Format: 565a340.pdf

Chemical Papers 56 (5) 340–344 (2002)