Fonvielle Matthieu, Therisod Helene, Hemery Marion, Therisod Michel
Equipe Chimie Bioorganique et Bioinorganique, ICMMO, Univ Paris-Sud, UMR 8182, F-91405 Orsay, France.
Bioorg Med Chem Lett. 2007 Jan 15;17(2):410-3. doi: 10.1016/j.bmcl.2006.10.030. Epub 2006 Oct 17.
We report the synthesis and biochemical evaluation of new competitive inhibitors of the cytosolic (NADH-dependent) glycerophosphate dehydrogenase. The best tested compound, phosphono-propionohydroxamic acid, with a Ki of 6 microM, might be of interest as an anti-obesity drug.
我们报告了胞质(依赖NADH的)磷酸甘油脱氢酶新竞争性抑制剂的合成及生化评估。测试效果最佳的化合物——膦酰基丙酰异羟肟酸,其抑制常数为6微摩尔,有望成为一种抗肥胖药物。