Synthesis and pharmacological study of antiarrhythmic activity of quaternary derivatives of trimecaine

Synthesis and antiarrhythmic activity of quaternary derivatives and mineral salts of diethylaminoacetic acid ortho-toluidide

“…The therapeutic effect of lidocaine and its analog trimecaine (monomecaine belongs to this series) is known to be short-lived because of rapid destruction in the liver [4]. Further research showed that preparation of quaternary ammonium derivatives based on the aforementioned local anesthetics increases the effectiveness and duration of their antiarrhythmic action [5 -8].Diethylaminoacetic acid o-toluidide [9] and quaternary derivatives (QD) based on it were synthesized as before [4] in order to investigate their antiarrhythmic activity. Alkylation of diethylaminoacetic acid o-toluidide by various halogen-containing normal alkanes, alkenes, and arylalkanes by heating in acetone produced its QD.…”

“…The therapeutic effect of lidocaine and its analog trimecaine (monomecaine belongs to this series) is known to be short-lived because of rapid destruction in the liver [4]. Further research showed that preparation of quaternary ammonium derivatives based on the aforementioned local anesthetics increases the effectiveness and duration of their antiarrhythmic action [5 -8].…”

“…Diethylaminoacetic acid o-toluidide [9] and quaternary derivatives (QD) based on it were synthesized as before [4] in order to investigate their antiarrhythmic activity. Alkylation of diethylaminoacetic acid o-toluidide by various halogen-containing normal alkanes, alkenes, and arylalkanes by heating in acetone produced its QD.…”