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

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 pr...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-09, Vol.18 (18), p.4929-4931
Hauptverfasser: 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.
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Sprache:eng
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Zusammenfassung: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.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.08.060