ChemInform Abstract: Synthesis and Pharmacological Evaluation of New (Indol‐3‐yl)alkylamides and Alkylamines Acting as Potential Serotonin Uptake Inhibitors.

Abstract

Synthesis and Pharmacological Evaluation of New (Indol-3-yl)alkylamides and Alkylamines Acting as Potential Serotonin Uptake Inhibitors.-In order to obtain novel 5-hydroxytryptamine (5-HT) uptake inhibitors, the indolylalkylamides (III), (V), and (VI) and alkylamines (VII) are prepared. The affinity of these compounds for 5-HT uptake sites is measured. Sixteen amides are studied but amide (VI) shows a moderate 5-HT uptake inhibitory effect. Although indolylalkylamines (VII) are about 17-fold less active than indalpine they demonstrate excellent selectivity for the 5-HT uptake site versus the dopamine uptake site. Compound (VIIb) is of interest because of possible antidepressant activity through selective inhibition of central neuronal serotonin uptake.