Xiang Jason, Ipek Manus, Suri Vipin, Tam May, Xing Yuzhe, Huang Nelson, Zhang Yanling, Tobin James, Mansour Tarek S, McKew John
Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, MA 02140, USA.
Bioorg Med Chem. 2007 Jul 1;15(13):4396-405. doi: 10.1016/j.bmc.2007.04.035. Epub 2007 Apr 25.
The design, synthesis, and biological evaluation of beta-keto sulfones as 11beta-HSD1 inhibitors and the mechanism of inhibition are described here. This class of compounds is not active against 11beta-HSD2 and therefore may have therapeutic potential for metabolic syndrome and type 2 diabetes.
本文描述了β-酮砜作为11β-羟基类固醇脱氢酶1（11β-HSD1）抑制剂的设计、合成及生物学评价，以及抑制机制。这类化合物对11β-羟基类固醇脱氢酶2（11β-HSD2）无活性，因此可能对代谢综合征和2型糖尿病具有治疗潜力。
