NOVEL PHOSPHORUS ORGANIC COMPOUNDS AS POTENTIAL ANESTHETICS

Abstract

For searching the novel classes of compounds with high biological activity and low toxicityfluorine containing α-aminophosphonates synthesized in conditions of one-pot Kabachnik-Fields reaction by interaction of 1-benzhydrylpiperazine, dimethylphosphite and p-, m- or o-fluorobenzaldehyde, had been tested on two models of local anesthetic activity and acute toxicity. It had turned out that the fluorine-containing α-aminophosphonates in varying degrees cause infiltration and conduction anesthesia and they are less toxic in comparison with the medicinesas trimecain, lidocaine and novocaine.It had been shown that aminophosphonate with fluorine in the o-position is the most active in models of infiltration and conduction anesthesia, the m-isomer - less active, the p-isomer locates in an intermediate position.

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