New semisynthetic quassinoids with in vivo antimalarial activity

Nobutoshi Murakami, Masanori Sugimoto, Motoyuki Kawanishi, Satoru Tamura, Hye Sook Kim, Khurshida Begum, Yusuke Wataya, Motomasa Kobayashi

Research output: Contribution to journalArticle

25 Citations (Scopus)

Abstract

On the basis of a comparative analysis for stability in mouse serum between 15-O-acetylbruceolide and bruceolide 15-methyl carbonate, several 3,15-dialkyl carbonates of bruceolide were synthesized and their in vitro antimalarial activity was assessed. Methyl, ethyl, and isopropyl carbonates with pronounced in vitro activity were further evaluated for in vivo antimalarial potency. Both the methyl and ethyl carbonates significantly increased the life span of mice as compared with 3,15-di-O-accetylbruceolide and chloroquine.

Original languageEnglish
Pages (from-to)638-641
Number of pages4
JournalJournal of Medicinal Chemistry
Volume46
Issue number4
DOIs
Publication statusPublished - 2003 Feb 13

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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