基于四氢喹啉的三环胺作为5-羟色胺受体的强效和选择性激动剂。
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT receptor.
作者信息
Schrader Thomas O, Kasem Michelle, Ren Albert, Feichtinger Konrad, Al Doori Bilal, Wei Jing, Wu Chunrui, Dang Huong, Le Minh, Gatlin Joel, Chase Kelli, Dong Jenny, Whelan Kevin T, Sage Carleton, Grottick Andrew J, Semple Graeme
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. 2016 Dec 15;26(24):5877-5882. doi: 10.1016/j.bmcl.2016.11.016. Epub 2016 Nov 9.
The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT receptor agonists are reported. An early lead containing a highly unique 6,6,7-ring system was optimized for both in vitro potency and selectivity at the related 5-HT receptor. Orally bioactive, potent, and selective 6,6,6-tricyclic 5-HT agonists were identified.
报道了基于四氢喹啉的三环胺作为5-羟色胺（5-HT）受体激动剂的合成、构效关系（SARs）及生物活性。对一种含有高度独特的6,6,7-环系统的早期先导化合物进行了优化，以提高其在相关5-HT受体上的体外效力和选择性。确定了具有口服生物活性、强效且选择性的6,6,6-三环5-HT激动剂。
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