Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.

  title={Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.},
  author={Jos{\'e} N. Dominguez and Caritza Le{\'o}n and Juan Abel Rodrigues and Neira Gamboa de Dom{\'i}nguez and Jiri Gut and Philip J. Rosenthal},
  journal={Journal of medicinal chemistry},
  volume={48 10},
Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteine protease falcipain-2, in vitro globin hydrolysis, beta-hematin formation, and murine Plasmodium berghei malaria. The most active antimalarial compound was 1-[3'-N-(N'-phenylurenyl)phenyl]-3(3,4,5-trimethoxyphenyl)-2-propen-1-one 49, with an IC(50) of 1.76 microM for inhibition of P. falciparum development… CONTINUE READING

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