51254-62-7Relevant articles and documents
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.
, p. 3878 - 3882 (2017)
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.
SUBSTITUTED PYRIMIDINES
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Page/Page column 100, (2013/04/10)
Disclosed are substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
Preparation of Certain Pyridopyrimidinones and Related Compounds as Candidate Fluorescent Probes for Hypoxic Cells in Solid Tumours
Parrick, John,Rarl, Harshad K.
, p. 2411 - 2433 (2007/10/02)
Non-fluorescent 3-nitropyridopyrimidin-4-ones have been prepared as potential molecular probes for hypoxia in solid tumours.Reduction of the nitro group was expected to occur in the hypoxic cells to give the corresponding fluorescent amino compounds.These amino compounds, produced by chemical reduction, were indeed fluorescent and some showed the desired large Stokes shifts together with an emitted light wavelength suitable for use in flow cytometry but the fluorescence quantum yields could be obtained in this series of compounds.
