Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4

Vincent P Rocco; Patrick G Spinazze; Todd J Kohn; Nicholas A Honigschmidt; David L Nelson; D Bradley Wainscott; Laura J Ahmad; Janice Shaw; Penny G Threlkeld; David T Wong; Kumiko Takeuchi

doi:10.1016/j.bmcl.2004.02.088

Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4

Bioorg Med Chem Lett. 2004 May 17;14(10):2653-6. doi: 10.1016/j.bmcl.2004.02.088.

Authors

Vincent P Rocco¹, Patrick G Spinazze, Todd J Kohn, Nicholas A Honigschmidt, David L Nelson, D Bradley Wainscott, Laura J Ahmad, Janice Shaw, Penny G Threlkeld, David T Wong, Kumiko Takeuchi

Affiliation

¹ Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA.

PMID: 15109671
DOI: 10.1016/j.bmcl.2004.02.088

Abstract

A series of 1-(1H-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.

MeSH terms

Antidepressive Agents, Second-Generation / chemical synthesis*
Antidepressive Agents, Second-Generation / pharmacology
Heterocyclic Compounds, 4 or More Rings / chemical synthesis
Heterocyclic Compounds, 4 or More Rings / pharmacology
Propanols / chemical synthesis
Propanols / pharmacology*
Protein Binding
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
Selective Serotonin Reuptake Inhibitors / pharmacology
Serotonin 5-HT1 Receptor Antagonists*
Stereoisomerism
Structure-Activity Relationship

Substances

Antidepressive Agents, Second-Generation
Heterocyclic Compounds, 4 or More Rings
Propanols
Serotonin 5-HT1 Receptor Antagonists
Serotonin Uptake Inhibitors