期刊
ARCHIV DER PHARMAZIE
卷 340, 期 7, 页码 339-344出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.200700013
关键词
conformationally restrained analogues; fosmidomycin; malaria tropica; Plasmodium falciparum
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.
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