Total Synthesis, and Antimalarial Activity of Symplostatin 4
Total Synthesis, and Antimalarial Activity of Symplostatin 4
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DOI：
10.1021/ol1024663
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发表时间：
2010-12-03
期刊：
影响因子：
5.2
通讯作者：
Payne, Richard J.
中科院分区：
文献类型：
--
作者：
Conroy, Trent;Guo, Jin T.;Payne, Richard J.
首次全合成了一种海洋蓝藻衍生的天然产物合丝菌素4。该路线的显着特点包括三个关键片段的有效制备和最终组装的天然产物通过顺序酰亚胺和酰胺偶联。还证明了Symplostatin 4具有显著的抗疟活性（对恶性疟原虫，菌株3D7的ED 50为74 nM）。
The first total synthesis of symplostatin 4, a marine cyanobacterium-derived natural product, is described. Notable features of the route include the efficient preparation of three key fragments and final assembly to the natural product via sequential imide and amide couplings. Symplostatin 4 was also demonstrated to possess significant antimalarial activity (ED50 of 74 nM against Plasmodium falciparum, strain 3D7).