Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1551-4. doi: 10.1016/j.bmcl.2010.01.082. Epub 2010 Jan 25.
Inhibition of 11beta-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11beta-HSD1 inhibitors. Highly potent compounds exhibiting inhibitory activities at both human and mouse 11beta-HSD1 were identified. Several compounds demonstrated significant in vivo activity in the mouse cortisone challenge assay.
抑制 11β-HSD1 在治疗代谢综合征的各种组分方面具有潜力。本文报道了新型氮杂双环磺酰胺类 11β-HSD1 抑制剂的发现。鉴定出对人和鼠 11β-HSD1 均具有抑制活性的高活性化合物。一些化合物在小鼠皮质酮挑战试验中表现出显著的体内活性。
