Exploration of a new type of antimalarial compounds based on febrifugine

Haruhisa Kikuchi, Keisuke Yamamoto, Seiko Horoiwa, Shingo Hirai, Ryota Kasahara, Norimitsu Hariguchi, Makoto Matsumoto, Yoshiteru Oshima

研究成果: Article査読

144 被引用数 (Scopus)


Febrifugine (1), a quinazoline alkaloid, isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. The use of 1 as an antimalarial drug has been precluded because of side effects, such as diarrhea, vomiting, and liver toxicity. However, the potent antimalarial activity of 1 has stimulated medicinal chemists to pursue compounds derived from 1, which may be valuable leads for novel drugs. In this study, we synthesized a new series of febrifugine derivatives formed by structural modifications at (i) the quinazoline ring, (ii) the linker, or (iii) the piperidine ring. Then, we evaluated their antimalarial activities. Thienopyrimidine analogue 15 exhibited a potent antimalarial activity and a high therapeutic selectivity both in vitro and in vivo, suggesting that 15 is a good antimalarial candidate.

ジャーナルJournal of Medicinal Chemistry
出版ステータスPublished - 2006 7月 27

ASJC Scopus subject areas

  • 分子医療
  • 創薬


「Exploration of a new type of antimalarial compounds based on febrifugine」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。