1-（4-苯氧基哌啶-1-基）-2-芳基氨基乙酮硬脂酰辅酶A去饱和酶1抑制剂的发现
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
作者信息
Zhao Hongyu, Serby Michael D, Smith Harriet T, Cao Ning, Suhar Tom S, Surowy Teresa K, Camp Heidi S, Collins Christine A, Sham Hing L, Liu Gang
机构信息
Metabolic Disease Research, Global Pharmaceutical Research and Development, R4MC, AP-10, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3388-91. doi: 10.1016/j.bmcl.2007.03.099. Epub 2007 Apr 5.
A series of novel stearoyl-CoA desaturase 1 (SCD1) inhibitors were identified by scaffold design based on known SCD1 inhibitors. Large structural changes were made leading to multiple analogs with comparable or improved potency. This approach is valuable for generation of proprietary compounds without conducting a costly high-throughput screening.
基于已知的硬脂酰辅酶A去饱和酶1（SCD1）抑制剂，通过骨架设计鉴定出了一系列新型SCD1抑制剂。进行了大规模的结构改变，从而产生了多种具有相当或更高活性的类似物。这种方法对于在不进行昂贵的高通量筛选的情况下生成专利化合物很有价值。
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