3-芳基-4-羟基喹啉-2(1H)-酮衍生物作为I型脂肪酸合酶抑制剂
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
作者信息
Rivkin Alexey, Kim Yoona R, Goulet Mark T, Bays Nathan, Hill Armetta D, Kariv Ilona, Krauss Stefan, Ginanni Nicole, Strack Peter R, Kohl Nancy E, Chung Christine C, Varnerin Jeffrey P, Goudreau Paul N, Chang Amy, Tota Michael R, Munoz Benito
机构信息
Department of Chemistry, Merck Research Laboratories, Boston, MA 02115, USA.
出版信息
Bioorg Med Chem Lett. 2006 Sep 1;16(17):4620-3. doi: 10.1016/j.bmcl.2006.06.014. Epub 2006 Jun 19.
A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC(50) = 1.4 microM, SAR studies led to compounds with more than 70-fold increase in potency (IC(50) < 20 nM).
制备了一系列具有脂肪酸合酶抑制活性的3-芳基-4-羟基喹啉-2(1H)-酮。从一种IC(50) = 1.4 microM的衍生物开始，通过构效关系研究得到了活性提高70多倍（IC(50) < 20 nM）的化合物。
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