Interconvertible geometric isomers of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors exhibit multiple binding modes

McConkey, Glenn A.; Bedingfield, Paul T.P.; Burrell, David R.; Chambers, Nicholas C.; Cunningham, Fraser; Prior, Timothy J.; Fishwick, Colin W.G.; Boa, Andrew N.

doi:10.1016/j.bmcl.2017.06.052

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Interconvertible geometric isomers of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors exhibit multiple binding modes (2017)
Journal Article
McConkey, G. A., Bedingfield, P. T., Burrell, D. R., Chambers, N. C., Cunningham, F., Prior, T. J., Fishwick, C. W., & Boa, A. N. (2017). Interconvertible geometric isomers of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors exhibit multiple binding modes. Bioorganic and Medicinal Chemistry Letters, 27(16), 3878-3882. https://doi.org/10.1016/j.bmcl.2017.06.052

Two new tricyclic β-aminoacrylate derivatives (2e and 3e) have been found to be inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) with Ki 0.037 and 0.15 μM respectively. 1H and 13C NMR spectroscopic data show that these compo... Read More about Interconvertible geometric isomers of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors exhibit multiple binding modes.