新型（R）-6,6a,7,8,9,10-六氢-5H-吡嗪并[1,2-a][1,n]萘啶作为 5-HT 受体的有效和选择性激动剂。
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 receptor.
机构信息
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2021 Apr 15;38:127872. doi: 10.1016/j.bmcl.2021.127872. Epub 2021 Feb 23.
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.
一系列新型（R）-6,6a,7,8,9,10-六氢-5H-吡嗪并[1,2-a][1,n]萘啶被鉴定为 5-HT 受体的有效和选择性激动剂。对先前报道的一系列外消旋四氢喹啉基三环胺进行优化，得到了一种先进的药物先导化合物（R）-4-（3,3,3-三氟丙基）-6,6a,7,8,9,10-六氢-5H-吡嗪并[1,2-a][1,8]萘啶，其具有优异的体外和体内药理学特性。
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