Abstract: Novel quinoline derivatives were prepared and evaluated their pharmaceutical activities. The quinoline derivatives according to the present invention effectively bind serotonin transporter (SERT) which is called serotonin reuptake site. Serotonin is one of the neurotransmitter and the lack of its concentration in synapse cause the depression. The quinoline derivatives in this invention can interrupt reuptake of serotonin into presynaptic neuron resulting the increasement of concentration of serotonin in synapse as well as stimulating the signal through the binding with serotonin recepter. Thus, they can be used for the prevention and treatment of mental disorder, especially depression, caused by the deficiency of serotonin concentration in synapse.