Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies.

@article{Guantai2011EnoneAC,
  title={Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies.},
  author={Eric M. Guantai and Kanyile K Ncokazi and Timothy J Egan and Jiri Gut and Philip J. Rosenthal and Ravi Bhampidipati and Anitha Kopinathan and Peter J. Smith and Kelly Chibale},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 10},
  pages={3637-49}
}
Analogues of the previously reported antimalarial hybrid compounds 8b and 12 were proposed with the aim of identifying compounds with improved solubility and retained antimalarial potency. In silico characterization predicted improved solubilities of the analogues, particularly at low pH; they retained acceptable predicted permeability properties but were predicted to be susceptible to hepatic metabolism. These analogues were synthesized and found to exhibit notable in vitro antimalarial… CONTINUE READING

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