Discovery and Early Clinical Research, Sunovion Pharmaceuticals Inc, 84 Waterford Drive, Marlborough, MA 01752, USA.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):520-3. doi: 10.1016/j.bmcl.2010.10.086. Epub 2010 Oct 28.
The present work describes a series of novel tetrahydroquinoline amines that potently inhibit the in vitro reuptake of serotonin and dopamine (dual reuptake inhibitors). The compounds are structurally related to a series we disclosed previously, but are improved with respect to cytochrome P-450 enzyme (CYP) and potassium ion channel Kv11.1 (hERG) inhibition and synthetic accessibility. The detailed synthesis and in vitro activity and ADME profile of the compounds is described, which represent a previously undisclosed dual reuptake inhibitor chemotype.
本工作描述了一系列新型四氢喹啉胺，它们能有效地抑制血清素和多巴胺的再摄取（双重再摄取抑制剂）。这些化合物与我们之前披露的一系列化合物在结构上相关，但在细胞色素 P-450 酶（CYP）和钾离子通道 Kv11.1（hERG）抑制以及合成可及性方面得到了改善。详细描述了化合物的合成、体外活性和 ADME 概况，它们代表了一种以前未公开的双重再摄取抑制剂化学型。
