4-双环杂芳基-哌啶衍生物作为有效的、口服生物利用的硬脂酰辅酶 A 去饱和酶-1（SCD1）抑制剂。第 1 部分：基于脲的类似物。
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.
机构信息
Cardiovascular and Metabolism Research, Janssen Research and Development, LLC, Welsh & McKean Roads, Spring House, PA 19477, USA.
出版信息
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6773-6. doi: 10.1016/j.bmcl.2013.09.096. Epub 2013 Oct 9.
PMID:24153205
Abstract
A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure-activity relationships focused on bicyclic heteroarenes and aminothiazole-urea portions are discussed. A trend of dose-dependent decrease in body weight gain in diet-induced obese (DIO) mice is also demonstrated.
摘要
本文描述了一系列新型基于尿素的 4-双环杂芳基-哌啶衍生物，它们是有效的 SCD1 抑制剂。讨论了结构活性关系，重点是双环杂芳环和氨噻唑-脲部分。还证明了在饮食诱导肥胖（DIO）小鼠中，体重增加呈剂量依赖性下降的趋势。
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