Facile synthesis of antimalarial 1,2-disubstituted 4-quinolones from 1,3-bisaryl-monothio-1,3-diketones

Ajjampura C. Vinayaka, Maralinganadoddi P. Sadashiva, Xianzhu Wu, Sergei S. Biryukov, José A. Stoute, Kanchugarakoppal S. Rangappa, D. Channe Gowda

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27 Scopus citations


A new strategy was developed to synthesize 1,2-disubstituted 4-quinolones in good yield starting from 1,3-bisaryl-monothio-1,3-diketone substrates. The synthesized compounds were evaluated for antimalarial activity using Plasmodium falciparum strains. All compounds, except for two, showed good activity. Of these, seven compounds exhibited an excellent antimalarial activity (IC50, <2 μM). More importantly, all seven compounds were equally effective in inhibiting the growth of both chloroquine-sensitive and chloroquine-resistant strains. The cytotoxicity assessment using carcinoma and non-carcinoma human cell lines revealed that almost all synthesized compounds were minimally cytotoxic (IC50, >50 μM).

Original languageEnglish (US)
Pages (from-to)8555-8561
Number of pages7
JournalOrganic and Biomolecular Chemistry
Issue number42
StatePublished - Nov 14 2014

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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