Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT 1A receptor antagonism/SSRI activities. Part 4

• Published in: Bioorganic & medicinal chemistry letters Vol. 14; no. 10; pp. 2653 - 2656
• Main Authors: Rocco, Vincent P., Spinazze, Patrick G., Kohn, Todd J., Honigschmidt, Nicholas A., Nelson, David L., Bradley Wainscott, D., Ahmad, Laura J., Shaw, Janice, Threlkeld, Penny G., Wong, David T., Takeuchi, Kumiko
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 2004
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2004.02.088

A series of 1-(1 H-indol-4-yloxy)-3-(4-arylpiperidinyl)propan-2-ols possessing potent dual 5-HT 1A receptor antagonism and serotonin reuptake inhibition was discovered. The fused aryl ring moiety contributed to the robust dual activities irrespective of the regiochemistry associated with its connectivity to the piperidine central ring. A series of 1-(1 H-indol-4-yloxy)-3-(4-arylpiperidinyl)propan-2-ols possessing potent dual 5-HT 1A receptor antagonism and serotonin reuptake inhibition was discovered. The fused aryl ring moiety contributed to the robust dual activities irrespective of the regiochemistry associated with its connectivity to the piperidine central ring.