新型 4,4-二取代环己基苯甲酰胺衍生物的合成与优化及其作为高效 11β-HSD1 抑制剂的研究。
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
机构信息
Amgen Inc, 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):405-10. doi: 10.1016/j.bmcl.2010.10.129. Epub 2010 Oct 31.
PMID:21093258
Abstract
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.
摘要
描述了一系列 4,4-二取代环己基苯甲酰胺 11β-HSD1 抑制剂的合成和 SAR 研究。优化过程迅速得到了具有高活性、高选择性和口服生物利用度的抑制剂，在大鼠和非人灵长类动物的体外药效模型中均显示出疗效。
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