Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT 2C receptor

A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT receptor. Optimizations performed on a previously reported series of racemic tetrahydroquinoline-based tricyclic amines, delivered an advanced drug lead, (...

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Published inBioorganic & medicinal chemistry letters Vol. 38; p. 127872
Main Authors Schrader, Thomas O, Zhu, Xiuwen, Kasem, Michelle, Ren, Albert, Liu, Chunyan, Wu, Chunrui, Dang, Huong, Le, Minh, Gatlin, Joel, Chase, Kelli, Frazer, John, Whelan, Kevin T, Grottick, Andrew J, Hutton, Clayton, Barden, Jeremy, Chen, Chuan, Ortiz, Alvaro, Feichtinger, Konrad, Semple, Graeme
Format Journal Article
LanguageEnglish
Published England 15.04.2021
Subjects
CNS drugs
Naphthyridine
5-HT(2C) agonists
Tricyclic amines
Lorcaserin
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Summary:A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT receptor. Optimizations performed on a previously reported series of racemic tetrahydroquinoline-based tricyclic amines, delivered an advanced drug lead, (R)-4-(3,3,3-trifluoropropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine, which displayed excellent in vitro and in vivo pharmacological profiles.
ISSN:1464-3405