Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: A new class of selective norepinephrine reuptake inhibitors

• Published in: Bioorganic & medicinal chemistry 2008-09, Vol.18 (18), p.4929-4931
• Main Authors: McComas, Casey C., Vu, An T., Mahaney, Paige E., Cohn, Stephen T., Fensome, Andrew, Marella, Michael A., Nogle, Lisa, Trybulski, Eugene J., Ye, Fei, Zhang, Puwen, Alfinito, Peter, Bray, Jenifer, Johnston, Grace, Koury, Elizabeth, Deecher, Darlene C.
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Catecholaminergic system; Humans; Indoles - chemical synthesis; Indoles - chemistry; Indoles - pharmacology; Medical sciences; Molecular Structure; Neuropharmacology; Neurotransmitter Uptake Inhibitors - chemical synthesis; Neurotransmitter Uptake Inhibitors - chemistry; Neurotransmitter Uptake Inhibitors - pharmacology; Neurotransmitters. Neurotransmission. Receptors; Norepinephrine - antagonists & inhibitors; Pharmacology. Drug treatments; Stereoisomerism; Structure-Activity Relationship
• ISSN: 0960-894X; 0968-0896; 1464-3405; 1464-3391
• DOI: 10.1016/j.bmcl.2008.08.060

A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones displays potent norepinephrine reuptake inhibition while maintaining good selectivity (>100-fold) against the human serotonin and dopamine transporters. Norepinephrine and serotonin play an important role in a wide variety of biological processes and are implicated in a number of neurological disorders. A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones was designed and synthesized that displays potent norepinephrine reuptake inhibition while maintaining high selectivity (>100-fold) against the human serotonin and dopamine transporters.