Bioorganic and Medicinal Chemistry Letters p. 3878 - 3882 (2017)
Update date:2022-08-02
Topics:
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.
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 compounds undergo ready cis-trans isomerisation at room temperature in polar solvents. In silico docking studies indicate that for both molecules there is neither conformation nor double bond configuration which bind preferentially to PfDHODH. This flexibility is favourable for inhibitors of this channel that require extensive positioning to reach their binding site.
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