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Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Aug 01; Vol. 19 (15), pp. 4031-3. Date of Electronic Publication: 2009 Jun 13. - Publication Year :
- 2009
-
Abstract
- A series of racemic 3-(trans-2-aminomethylcyclopentyl)indoles was synthesized and found to have potent binding to the human serotonin transporter (hSERT). The most active analog was synthesized stereospecifically and the active enantiomer was shown to have high affinity binding to hSERT.
- Subjects :
- Animals
Antidepressive Agents chemistry
Chemistry, Pharmaceutical methods
Cyclopentanes chemistry
Dose-Response Relationship, Drug
Humans
Inhibitory Concentration 50
Ligands
Models, Chemical
Protein Binding
Rats
Serotonin chemistry
Selective Serotonin Reuptake Inhibitors chemistry
Structure-Activity Relationship
Indoles chemistry
Selective Serotonin Reuptake Inhibitors pharmacology
Tryptamines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19560923
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.06.026