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.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 45, No. 8, pp. 22 – 25, August, 2011.
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Kayukova, L.A., Praliev, K.D., Akhelova, A.L. et al. Local anesthetic activity of new amidoxime derivatives. Pharm Chem J 45, 468–471 (2011). https://doi.org/10.1007/s11094-011-0657-0
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DOI: https://doi.org/10.1007/s11094-011-0657-0