Preparation and local anaesthetic activity of N-[2-(tert-amino)ethyl]- and N-(lupinyl)-benzotriazol-1/2-ylacetamides.
Two sets of N-[2-(tert-amino)ethyl]- and N-[(quinolizidin-1 alpha-yl) methyl]-benzotriazol-2-ylacetamides, bearing substituents on position 5 or 5 and 6, were prepared and tested for local anaesthetic activity in comparison with lidocaine. Most of the prepared compounds exhibited a fairly good activity comparable or superior to that of lidocaine. The introduction of substituents on the benzene ring and the replacement of the usual tert-amino alkyl chains with the quinolizidin-1 alpha-ylmethyl (lupinyl) moiety were quite profitable for both the intensity and duration of activity. One selected compound was subjected to a large pharmacological screening and found endowed with a good level of the purported antiarrhythmic activity without any other disturbing activity.
Vazzana
I
I
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Boido
A
A
Sparatore
F
F
Di Carlo
R
R
Raso
G M
GM
Pacilio
M
M
D000081:Acetamides / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000779:Anesthetics, Local / Q000737:chemistry / Q000633:toxicity; D000818:Animals; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
D000081:Acetamides; D000779:Anesthetics, Local; D014230:Triazoles