Thiazolopyrimidine Inhibitors of 2-Methylerythritol 2,4-Cyclodiphosphate Synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparum (pages 1092–1101)
Julie G. Geist, Susan Lauw, Victoria Illarionova, Boris Illarionov, Markus Fischer, Tobias Gräwert, Felix Rohdich, Wolfgang Eisenreich, Johannes Kaiser, Michael Groll, Christian Scheurer, Sergio Wittlin, José L. Alonso-Gómez, W. Bernd Schweizer, Adelbert Bacher and François Diederich
Article first published online: 17 MAY 2010 | DOI: 10.1002/cmdc.201000083
A thiazolopyrimidine derivative resulting from high-throughput screening was found to be active toward 2-methylerythritol 2,4-cyclodiphosphate synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparum, with respective IC50 values of 6.1±0.8 and 9.6±1.5 μM. Some of the prepared derivatives exhibit weak in vitro activity against the protozoan parasite P. falciparum.