Local anesthetic activity of new amidoxime derivatives

Abstract

Three series of amidoxime derivatives including nitrous derivatives of α-chloro-α-isonitrosoacetone and hydrochlorides of O-aroyl-β-aminopropioamidoximes and 3-[β-(piperidin-1-yl)]ethyl-5-aryl-1,2,4-oxadiazoles were tested for conduction, infiltration, and terminal anesthesia. There are four interesting “hit” compounds, i.e., the hydrochloride of O-m-chlorophenyl-β-(benzimidazol-1-yl)propioamidoxime (VII), the hydrochloride of O-p-nitrophenyl-β-(benzimidazol-1-yl)propioamidoxime (VIII), 3-[β-(piperidin-1-yl)]ethyl-5-p-tolyl-1,2,4-oxadiazole (IX), and 3-[β-(piperidin-1-yl)]ethyl-5-m-chlorophenyl-1,2,4-oxadiazole (X), which exhibit higher activity than the reference drugs (trimecaine, lidocaine, novocaine, kazcaine). As a whole, all tested compounds were active in conduction and infiltration anesthesia (at the level of the reference drugs) and did not show activity in terminal anesthesia. Compounds VII – X are of interest for further testing under condition and infiltration anesthesia conditions.