| 1469884-33-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• CAS: 1469884-33-0
• 化学式: C₁₉H₂₅N₇
• 分子量: 351.454
• InChiKey: YBLBRPQXTQFHLY-WKILWMFISA-N

反应信息

• 作为反应物：
  描述：

  对氟碘苯 、 在 copper(l) iodide 、 potassium carbonate 、 L-脯氨酸 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues

  摘要：

  The structural diversity and SAR in a series of imidazopyridazine inhibitors of Plasmodium falciparum calcium dependent protein kinase 1 (PfCDPK1) has been explored and extended. The opportunity to further improve key ADME parameters by means of lowering log D was identified, and this was achieved by replacement of a six-membered (hetero)aromatic linker with a pyrazole. A short SAR study has delivered key examples with useful in vitro activity and ADME profiles, good selectivity against a human kinase panel and improved levels of lipophilic ligand efficiency. These new analogues thus provide a credible additional route to further development of the series. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.08.010