I. Vazzana et al., PREPARATION AND LOCAL-ANESTHETIC ACTIVITY OF N-[2-(TERT-AMINO)ETHYL]-1 2-YLACETAMIDES AND N-(LUPINYL)-BENZOTRIAZOL-1/2-YLACETAMIDES/, Il Farmaco, 52(3), 1997, pp. 131-139
Two sets of N-[2-(tert-amino)ethyl]- and N-[(quinolizidin-1 alpha-yl)m
ethyl]-benzotriazol-2-ylacetamides, bearing substituents on position 5
or 5 and 6, were prepared and tested for local anaesthetic activity i
n comparison with lidocaine. Most of the prepared compounds exhibited
a fairly good activity comparable or superior to that of lidocaine. Th
e introduction of substituents on the benzene ring and the replacement
of the usual tert-amino alkyl chains with the quinolizidin-1 alpha-yl
methyl (lupinyl) moiety were quite profitable for both the intensity a
nd duration of activity. One selected compound was subjected to a larg
e pharmacological screening and found endowed with a good level of the
purported antiarrhythmic activity without any other disturbing activi
ty.