Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents

Kuldeep Patel, Chandrabose Karthikeyan, N. S. Hari Narayana Moorthy, Girdhar Singh Deora, Viswas Raja Solomon, Hoyun Lee, Piyush Trivedi

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A novel series of 3-cinnamoyl-4-hydroxy-2Hchromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4- nitrophenyl)acryloyl)-2Hchromen-2-one showed inhibitory potency (IC 50) of 3.1 and 4 μg/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy- 2H-chromen-2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance. 

Original languageEnglish
Pages (from-to)1780-1784
Number of pages5
JournalMedicinal Chemistry Research
Issue number8
Publication statusPublished - Aug 2012
Externally publishedYes


  • Antimalarial
  • Chalcones
  • Coumarin

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