双环和三环杂环衍生物作为组胺 H3 受体拮抗剂用于治疗肥胖症。
Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity.
机构信息
Department of Chemical Research, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2013 Nov 1;23(21):6004-9. doi: 10.1016/j.bmcl.2013.08.013. Epub 2013 Aug 19.
PMID:24035485
Abstract
A novel series of non-imidazole bicyclic and tricyclic histamine H3 receptor antagonists has been discovered. Compound 17 was identified as a centrally penetrant molecule with high receptor occupancy which demonstrates robust oral activity in rodent models of obesity. In addition compound 17 possesses clean CYP and hERG profiles and shows no behavioral changes in the Irwin test.
摘要
我们发现了一系列新型非咪唑类双环和三环组氨酸 H3 受体拮抗剂。化合物 17 被鉴定为一种具有高受体占有率的中枢穿透性分子，在肥胖症啮齿动物模型中具有良好的口服活性。此外，化合物 17 具有良好的 CYP 和 hERG 特性，且在 Irwin 试验中没有行为改变。
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