Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials.

  title={Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials.},
  author={Clive L Yeates and John F Batchelor and Edward C Capon and Neil J Cheesman and Mitch Fry and Alan T Hudson and Mary Pudney and Helen Trimming and James M Woolven and Jos{\'e} Mar{\'i}a Garc{\'i}a Bueno and Jes{\'u}s Chicharro and Esther Fern{\'a}ndez and Jos{\'e} Mar{\'i}a Fiandor and Domingo Gargallo-Viola and Federico G{\'o}mez de las Heras and Esperanza A Herreros and Mar{\'i}a L Le{\'o}n},
  journal={Journal of medicinal chemistry},
  volume={51 9},
A series of diaryl ether substituted 4-pyridones have been identified as having potent antimalarial activity superior to that of chloroquine against Plasmodium falciparum in vitro and murine Plasmodium yoelii in vivo. These were derived from the anticoccidial drug clopidol through a systematic study of the effects of varying the side chain on activity. Relative to clopidol the most active compounds show >500-fold improvement in IC50 for inhibition of P. falciparum in vitro and about 100-fold… CONTINUE READING

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