PREPARATION AND LOCAL-ANESTHETIC ACTIVITY OF N-[2-(TERT-AMINO)ETHYL]-1 2-YLACETAMIDES AND N-(LUPINYL)-BENZOTRIAZOL-1/2-YLACETAMIDES/

Citation
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
Citations number
36
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
ISSN journal
0014827X
Volume
52
Issue
3
Year of publication
1997
Pages
131 - 139
Database
ISI
SICI code
0014-827X(1997)52:3<131:PALAON>2.0.ZU;2-H
Abstract
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.