New semisynthetic quassinoids with in vivo antimalarial activity

  • J Med Chem. 2003 Feb 13;46(4):638-41. doi: 10.1021/jm0201971.
Nobutoshi Murakami  1 ,  Masanori Sugimoto ,  Motoyuki Kawanishi ,  Satoru Tamura ,  Hye-Sook Kim ,  Khurshida Begum ,  Yusuke Wataya ,  Motomasa Kobayashi
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
PMID: 12570385 DOI: 10.1021/jm0201971
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.