Conformationally restrained aromatic analogues of fosmidomycin and FR900098

Conformationally restrained aromatic analogues of fosmidomycin and FR900098
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DOI:
10.1002/ardp.200700013
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发表时间:
2007-07-01
影响因子:
5.1
通讯作者:
Walter, Rolf D.
Walter, Rolf D.
中科院分区:
医学3区
文献类型:
--
作者:
Kurz, Thomas;Schlueter, Katrin;Walter, Rolf D.

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The synthesis and in-vitro antimalarial activity of conformationally restrained bis(pivaloyloxymethyl) ester analogues of the natural product fosmidomycin is presented. In contrast to alpha-aryl-substituted analogues, conformationally restrained aromatic analogues exhibit only moderate in-vitro antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. The most active derivative displays an IC50 value of 47 mu M.