Synthesis and biological evaluation of novel 6-nitro-5-substituted aminoquinolines as local anesthetic and anti-arrhythmic agents: molecular modeling study

A series of 6-nitro-5-[1-oxo-2-(substituted amino)ethylamino and 2-(substituted amino) propylamino] quinoline (4a-i and 5a-i) was synthesized and evaluated for their local anesthetic and anti-arrhythmic activity. The detailed synthesis, spectroscopic, and biological data are reported. Molecular modeling methods are used to study the local anesthetic activity of lidocaine and the active compounds by means of the AM1 method. The superposition of the stable conformations of these compounds was studied using the HyperChem 5.11 program. (c) 2005 Elsevier Ltd. All rights reserved.