NEW ARYLPIPERAZINE DERIVATIVES WITH HIGH-AFFINITY FOR 5-HT3 RECEPTOR-SITES

The synthesis and 5-HT3 affinities of 3- and 4-substituted -2-(1-piper azinyl) or -(4-methyl-1-piperazinyl)quinoline are reported. These comp ounds display higher affinities than derivatives from the same chemica l family, such as quipazine or 7-(4-methyl-1-piperazinyl)-6H-[1] benzo pyrano[3,4-c]quinoline 3c. For a better understanding of the conformat ional behavior of these new arylpiperazine derivatives in their intera ction with the 5-HT3 recognition sites, a computational study is prese nted, which shows the importance of steric hindrance at the 3-position of the quinoline ring.