Synthesis and biological evaluation of 1, 4-naphthoquinones and quinoline-5, 8-diones as antimalarial and schistosomicidal agents

…, K Becker, DL Williams, E Davioud-Charvet

Index: Lanfranchi, Don Antoine; Cesar-Rodo, Elena; Bertrand, Benoit; Huang, Hsin-Hung; Day, Latasha; Johann, Laure; Elhabiri, Mourad; Becker, Katja; Williams, David L.; Davioud-Charvet, Elisabeth Organic and Biomolecular Chemistry, 2012 , vol. 10, # 31 p. 6375 - 6387

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Citation Number: 23

Abstract

Improving the solubility of polysubstituted 1, 4-naphthoquinone derivatives was achieved by introducing nitrogen in two different positions of the naphthoquinone core, at C-5 and at C-8 of menadione through a two-step, straightforward synthesis based on the regioselective hetero-Diels–Alder reaction. The antimalarial and the antischistosomal activities of these polysubstituted aza-1, 4-naphthoquinone derivatives were evaluated and led to the ...