期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 10, 期 31, 页码 6375-6387出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob25812a
关键词
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资金
- US NIH/National Institute of Allergy and Infectious Disease (NIAID) [R01AI065622]
- NIH
- DFG [SFB 544, BE1540-15-1]
- Centre National de la Recherche Scientifique (CNRS)
- University of Strasbourg [UMR 7509 CNRS-UdS]
- International Center for Frontier Research in Chemistry (ic-FRC) in Strasbourg
- NIH/NIAID [HHSN272201000005I]
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 selection of distinct compounds for antimalarial versus antischistosomal action. The Ag-II-assisted oxidative radical decarboxylation of the phenyl acetic acids using AgNO3 and ammonium peroxodisulfate was modified to generate the 3-picolinyl-menadione with improved pharmacokinetic parameters, high antimalarial effects and capacity to inhibit the formation of beta-hematin.
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