咪唑并哒嗪类化合物作为新型疟疾激酶PfPK7抑制剂的合成及体外评价
Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7.
作者信息
Bouloc Nathalie, Large Jonathan M, Smiljanic Ela, Whalley David, Ansell Keith H, Edlin Christopher D, Bryans Justin S
机构信息
Drug Discovery Group, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, UK.
出版信息
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5294-8. doi: 10.1016/j.bmcl.2008.08.043. Epub 2008 Aug 19.
A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.
一项高通量筛选活动鉴定出多种咪唑并哒嗪类化合物是疟原虫激酶PfPK7的新型抑制剂。进一步的合成化学研究使得能够制备出一些具有良好体外活性的类似物。尽管这些化合物显示出可能具有广谱抑制活性，但它们是进一步化学优化的有用起点。
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