Pharmacochemistry of Novel Aminoketone Phthalimide, Δ4‐Tetrahydrophthalimide, and Arylsuccinimide Derivatives with Local Anaesthetic Activity

Abstract

A number of aminoketones with prospective local anaesthetic activity were prepared. The structure of the synthesized compounds was confirmed by spectroscopic and elemental analyses. The physiochemical parameters (pka and logP) were also investigated. The local anaesthetic activity was determined in vitro on sciatic frog's nerve by the compound action potential technique: the phthalimide derivatives possess considerable local anaesthetic activity equal to that of lidocaine and higher than that of procaine.