- Ozonation of substituted 2-thiouracils and pyrimidine-2-thione
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The ozonation of substituted 2-thiouracils and pyrimidine-2-thione is reported; this provides a new method for the synthesis of several pyrimidine derivatives.
- Crestini, Claudia,Saladino, Raffaele,Nicoletti, Rosario
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- Synthesis of febrifugine derivatives and development of an effective and safe tetrahydroquinazoline-type antimalarial
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Febrifugine, a quinazoline alkaloid isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. Although the use of ferifugine as an antimalarial drug has been precluded because of its severe side effects, its potent antimalarial activity has stimulated medicinal chemists to pursue its derivatives instead, which may provide valuable leads for novel antimalarial drugs. In the present study, we synthesized new derivatives of febrifugine and evaluated their in vitro and in vivo antimalarial activities to develop antimalarials that are more effective and safer. As a result, we proposed tetrahydroquinazoline-type derivative as a safe and effective antimalarial candidate.
- Kikuchi, Haruhisa,Horoiwa, Seiko,Kasahara, Ryota,Hariguchi, Norimitsu,Matsumoto, Makoto,Oshima, Yoshiteru
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- Oxidation of substituted 2-thiouracils and pyrimidine-2-thione with ozone and 3,3-dimethyl-1,2-dioxirane
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Ozone and 3,3-dimethyl-1,2-dioxirane react with substituted 2-thiouracils and pyrimidine-2-thione to afford several interesting desulfurized products. The effect of the solvent, protic as opposed to nonprotic, on the course of oxidation was striking.
- Claudia, Crestini,Mincione, Enrico,Saladino, Raffaele,Nicoletti, Rosario
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p. 3259 - 3272
(2007/10/02)
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