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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs
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4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs

机译:4-双环杂芳基-哌啶衍生物可作为有效的,口服生物利用的硬脂酰CoA去饱和酶1(SCD1)抑制剂。第1部分:基于尿素的类似物

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摘要

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.
机译:描述了一系列新的基于尿素的4-双环杂芳基-哌啶衍生物作为有效的SCD1抑制剂。讨论了结构-活性关系集中在双环杂芳烃和氨基噻唑-脲部分。还显示了饮食诱导的肥胖(DIO)小鼠体重增加的剂量依赖性下降趋势。

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