No abstract

The synthesis and in-vitro antimalarial activity of gamma-substituted bis(pivaloyloxymethyl)ester analogues of the drug candidate fosmidomycin have been investigated. In contrast to the high antimalarial activity of alpha-aryl substituted fosmidomycin analogues like alpha-phenylfosmidomycin, gamma-substituted derivatives display only weak to moderate activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum.

α-Phenylethyl substituted bis(pivaloyloxymethyl) ester analogues of the natural products Fosmidomycin and FR900098 have been synthesized, and their in vitro antimalarial activity determined. The α-phenylethyl substituted Fosmidomycin analogue displays moderate in vitro antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum.

Antibiotics U 1200 γ-Substituted Bis(pivaloyloxymethyl)ester Analogues of Fosmidomycin and FR900098. -The in vitro antimalarial activity of title compounds (VIII) is investigated. However, the γ-substituted analogues display only weak to moderate efects against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. -(KURZ*, T.; BEHRENDT, C.; PEIN, M.; KAULA, U.; BERGMANN, B.; WALTER, R. D.; Arch.