{Reference Type}: Journal Article
{Title}: 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-HT2C receptor.
{Author}: Schrader TO;Zhu X;Kasem M;Ren A;Liu C;Wu C;Dang H;Le M;Gatlin J;Chase K;Frazer J;Whelan KT;Grottick AJ;Hutton C;Barden J;Chen C;Ortiz A;Feichtinger K;Semple G;
{Journal}: Bioorg Med Chem Lett
{Volume}: 38
{Issue}: 0
{Year}: 04 2021 15
{Factor}: 2.94
{DOI}: 10.1016/j.bmcl.2021.127872
{Abstract}: 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-HT2C 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.