Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):411-6. doi: 10.1016/j.bmcl.2010.10.128. Epub 2010 Oct 30.
The development and synthesis of potent p38α MAP kinase inhibitors containing a pyridazinone platform is described. Evolution of the p38α selective pyridopyridazin-6-one series from the p38α/β dual inhibitor 2H-quinolizin-2-one series will be discussed in full detail.
描述了含有哒嗪酮平台的强效 p38α MAP 激酶抑制剂的开发和合成。将全面讨论 p38α/β 双重抑制剂 2H-喹啉-2-酮系列中 p38α 选择性哒嗪并哒嗪酮-6-酮系列的演变。