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. 2020 Feb;17(2):e1900597.
doi: 10.1002/cbdv.201900597. Epub 2020 Jan 16.

New Antiparasitic Bis-Naphthoquinone Derivatives

Jana Jentzsch  1 , Waleed S Koko  2 , Ibrahim S Al Nasr  2   3 , Tariq A Khan  4 , Rainer Schobert  5 , Klaus Ersfeld  1 , Bernhard Biersack  5
Affiliations

New Antiparasitic Bis-Naphthoquinone Derivatives

Jana Jentzsch et al. Chem Biodivers. 2020 Feb.

Abstract

A series of bis-naphthoquinone derivatives prepared by condensation of aryl aldehydes with lawsone were tested for antiparasitic activities against Toxoplasma gondii and Trypanosoma brucei parasites. Monofluorophenyl derivative 1a, 3,4-difluorophenyl analog 1c and furyl compound 1l exhibited significant activity against T. gondii cells and appear to be new promising drug candidates against this parasite. The 3,4,5-trifluorophenyl derivative 1g and the isovanillyl derivative 1j displayed selective activity against Leishmania major amastigotes.

Keywords: biological activity; fluorine; furan; lawsone; neglected tropical diseases; synthesis.

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References

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