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

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 connect...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-05, Vol.14 (10), p.2653-2656
Hauptverfasser:	ROCCO, Vincent P, SPINAZZE, Patrick G, TAKEUCHI, Kumiko, KOHN, Todd J, HONIGSCHMIDT, Nicholas A, NELSON, David L, WAINSCOTT, D. Bradley, AHMAD, Laura J, SHAW, Janice, THRELKELD, Penny G, WONG, David T
Format:	Artikel
Sprache:	eng
Schlagworte:	Antidepressive Agents, Second-Generation - chemical synthesis Antidepressive Agents, Second-Generation - pharmacology Biological and medical sciences Heterocyclic Compounds, 4 or More Rings - chemical synthesis Heterocyclic Compounds, 4 or More Rings - pharmacology Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Propanols - chemical synthesis Propanols - pharmacology Protein Binding Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Serotonin 5-HT1 Receptor Antagonists Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - pharmacology Serotoninergic system Stereoisomerism Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.02.088