金刚烷砜和磺酰胺类11-β-羟基类固醇脱氢酶1抑制剂。
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.
作者信息
Sorensen Bryan, Winn Martin, Rohde Jeff, Shuai Qi, Wang Jiahong, Fung Steven, Monzon Katina, Chiou William, Stolarik DeAnne, Imade Hovis, Pan Liping, Deng Xiaoqing, Chovan Linda, Longenecker Kenton, Judge Russell, Qin Wenying, Brune Michael, Camp Heidi, Frevert Ernst U, Jacobson Peer, Link J T
机构信息
Abbott, Dept. 47F, Bldg. AP-10, Rm. 301, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jan 15;17(2):527-32. doi: 10.1016/j.bmcl.2006.10.008. Epub 2006 Oct 7.
Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.
已发现强效且具选择性的11-β-羟基类固醇脱氢酶1（11-beta-HSD-1）金刚烷砜和磺酰胺抑制剂。这些系列中的选定化合物具有良好的药代动力学特征，口服给药后能在较长时间内强烈抑制肝脏、脂肪和大脑中的HSD1。
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