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

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 activ...

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Bibliographic Details
Published in:Organic & biomolecular chemistry 2014-11, Vol.12 (42), p.8555-8561
Main Authors: Vinayaka, Ajjampura C, Sadashiva, Maralinganadoddi P, Wu, Xianzhu, Biryukov, Sergei S, Stoute, José A, Rangappa, Kanchugarakoppal S, Gowda, D Channe
Format: Article
Language:English
Subjects:
4-Quinolones - chemical synthesis
4-Quinolones - chemistry
4-Quinolones - pharmacology
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Cell Line
Cell Line, Tumor
Humans
Malaria, Falciparum - drug therapy
Plasmodium
Plasmodium falciparum - drug effects
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Summary: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, 50 μM).
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob01455c