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

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 22; pp. 3939 - 3942
• Main Authors: Takeuchi, Kumiko, Kohn, Todd J, Honigschmidt, Nicholas A, Rocco, Vincent P, Spinazze, Patrick G, Atkinson, Steven T, Hertel, Larry W, Nelson, David L, Wainscott, D.Bradley, Ahmad, Laura J, Shaw, Janice, Threlkeld, Penny G, Wong, David T
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 2003
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2003.09.002

A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT 1A receptor antagonism and serotonin reuptake inhibition was discovered. Modification of potential metabolic sites of 1-(1 H-indol-4-yloxy)-3-(4-benzo[ b]thiophen-2-ylpiperidinyl)propan-2-ols further improved the in vitro binding affinities and functional antagonism. A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT 1A receptor antagonism and serotonin reuptake inhibition was discovered. Modification of potential metabolic sites of 1-(1 H-indol-4-yloxy)-3-(4-benzo[ b]thiophen-2-ylpiperidinyl)propan-2-ols further improved the in vitro binding affinities and functional antagonism.