噻吩并吡啶酮类化合物的发现与构效关系研究：一类小分子AMPK激活剂
Discovery and SAR development of thienopyridones: a class of small molecule AMPK activators.
作者信息
Zhao Gang, Iyengar Rajesh R, Judd Andrew S, Cool Barbara, Chiou William, Kifle Lemma, Frevert Ernst, Sham Hing, Kym Philip R
机构信息
Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3254-7. doi: 10.1016/j.bmcl.2007.04.011. Epub 2007 Apr 10.
AMP-activated protein kinase (AMPK) is well established as a sensor and regulator of intracellular and whole-body energy metabolism. A high-throughput screen was performed in order to identify chemotypes that are bound by AMPK. A novel thienopyridone compound (1) was identified and subsequently optimized. The structure-activity relationships that emerged from this effort are described.
AMP激活的蛋白激酶（AMPK）作为细胞内和全身能量代谢的传感器和调节剂已得到充分证实。为了鉴定与AMPK结合的化学类型，进行了高通量筛选。鉴定出一种新型噻吩并吡啶化合物（1），随后对其进行了优化。描述了由此产生的构效关系。
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