The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex
The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex
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DOI：
10.1039/c1md00183c
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发表时间：
2012-01-01
期刊：
影响因子：
--
通讯作者：
O'Neill, Paul M.
中科院分区：
文献类型：
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作者：
Cowley, Robin;Leung, Suet;O'Neill, Paul M.
使用Gould-Jacobs方法制备了一系列6-和7-取代的喹诺酮。类似物在7系列表达活性低至0.46 nM的恶性疟原虫疟疾寄生虫和对接研究中进行的计算机模拟在酵母Qo网站证明了一个关键作用的残基His 182和Glu 272的识别高效能的抑制剂。
Using the Gould-Jacobs methodology a small array of 6- and 7-substituted quinolones have been prepared. Analogues in the 7-series express activity as low as 0.46 nM versus Plasmodium falciparum malaria parasites and docking studies performed in silico at the yeast Qo site demonstrate a key role for residues His182 and Glu 272 in the recognition of high potency inhibitors.