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,Bioorganic & Medicinal Chemistry Letters

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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
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2021-02-23 , DOI: 10.1016/j.bmcl.2021.127872
Thomas O Schrader ₁ , Xiuwen Zhu ₁ , Michelle Kasem ₁ , Albert Ren ₁ , Chunyan Liu ₂ , Chunrui Wu ₂ , Huong Dang ₁ , Minh Le ₁ , Joel Gatlin ₁ , Kelli Chase ₁ , John Frazer ₁ , Kevin T Whelan ₁ , Andrew J Grottick ₁ , Clayton Hutton ₁ , Jeremy Barden ₁ , Chuan Chen ₁ , Alvaro Ortiz ₁ , Konrad Feichtinger ₁ , Graeme Semple ₁

Affiliation

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_2C 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.

中文翻译：

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-HT2C 受体的有效和选择性激动剂

一系列新型 ( R )-6,6a,7,8,9,10-hexahydro-5 H -pyrazino [1,2- a ][1,n]naphthyridines 被鉴定为 5- 的有效和选择性激动剂HT _2C受体。对先前报道的一系列基于外消旋四氢喹啉的三环胺进行优化，提供了一种先进的药物先导，( R )-4-(3,3,3-三氟丙基)-6,6a,7,8,9,10-六氢-5 H-吡嗪并[1,2- a ][1,8]萘啶，在体外和体内都显示出优异的药理学特性。

更新日期：2021-03-01

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