Synthesis of febrifugine derivatives and development of an effective and safe tetrahydroquinazoline-type antimalarial

Haruhisa Kikuchi, Seiko Horoiwa, Ryota Kasahara, Norimitsu Hariguchi, Makoto Matsumoto, Yoshiteru Oshima

研究成果: Article査読

38 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)10-19
ページ数10
ジャーナルEuropean Journal of Medicinal Chemistry
76
DOI
出版ステータスPublished - 2014 4月 9
外部発表はい

ASJC Scopus subject areas

  • 薬理学
  • 創薬
  • 有機化学

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