Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369494 | Bioorganic & Medicinal Chemistry Letters | 2016 | 6 Pages |
Abstract
The central role of the biogenic monoamine serotonin (5-hydroxytryptamine, 5-HT) as a neurotransmitter with important cognitive and behavioral functions is well known. However, 5-HT produced in the brain only accounts for approximately 5% of the total amount of 5-HT generated in the body. At the onset of our work, it appeared that substituted phenylalanine derivatives or related aryl amino acids were required to produce potent inhibitors of TPH1, as significant losses of inhibitory activity were noted in the absence of this structural element. We disclose herein the discovery of a new class of TPH1 inhibitors that significantly lower peripherally 5-HT.
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Related Topics
Physical Sciences and Engineering
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Organic Chemistry
Authors
Daniel R. Goldberg, Stéphane De Lombaert, Robert Aiello, Patricia Bourassa, Nicole Barucci, Qing Zhang, Vishwas Paralkar, James Valentine, William Zavadoski,